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Vaccinium myrtillus L. leaves contain bioactive components, such as polyphenols, stilbenes, iridoid glycosides, fatty acids, and fibers. However, polyphenols possess low solubility, stability, and bioavailability, thus the encapsulation of the mentioned active principles in different carriers is necessary. Liposomes are widely used as a carrier for the encapsulation, preservation, and controlled release of polyphenols in various products. Therefore, the aims of the presented research are the development and characterization of V. myrillus leaf extract-loaded liposomes via the determination of encapsulation efficiency, particle size, polydispersity index (PDI), zeta potential, and mobility.

By-products derived protein hydrolysates from Salmo salar are known to have important bioactivities such as antioxidative activity. However, their application in the food industry has been limited for a few reasons, including low bioavailability, low stability, heterogenous nature, interaction with food matrix and hydrophobicity. Nanoencapsulation can be employed as a strategy to overcome the above challenges that are faced by the peptides. Different types of carriers can be used for nanoencapsulation, including lipid-based, polysaccharide-based and protein-based. So this study consisted of two different delivery techniques developed for S.salar by-products derived protein hydrolysates (SPH). The objective of the first study was to optimize the process conditions (aqueous phase % in primary water in oil emulsion (W), aqueous phase% in w/o/w emulsion (W/O), PGPR 90% and Tween 80%) for W/O/W nanoemulsion preparation to encapsulate SPH. A Box-Benkan design was used to optimize the conditions for the emulsion preparation. Optimized conditions for emulsion preparation: W% =20%, W/O = 20%, PGPR = 8% and Tween 80 = 2.6% were obtained respectively. Experimented particle size and EE values under these conditions were 285.5 nm and 59%, respectively. Optimization of a double emulsion for encapsulating was achieved. Optimized emulsion and coated emulsions showed good storage ability over 28 days period. And the objective of the second study was to optimize the process conditions for chitosan/alginate nanoparticles (CS/AL NPs) to encapsulate SPH. Independent variables were alginate/chitosan (w/w), alginate/ CaCl2 (w/w) and alginate/ peptides (w/w) with three levels. The optimized nanoparticles’ particle size, zeta potential and encapsulation efficiency (EE) were 536.7 nm, -30.2 mV and 29.8 %, respectively. XRD and FTIR results proved the incorporation of SPH into the CS/AL NPs. Moreover, both systems showed a sustainable release of SPH in the gastrointestinal model conditions. T

Research background. Due to numerous health-promoting properties, dandelion has been used in traditional medicine as a herbal remedy, but also as a food product. Dandelion health benefits are ascribed to the presence of different bioactive compounds in its tissues, among which polyphenols play a significant role. However, the low stability of polyphenols is a critical parameter for their successful implementation into products. Thus, their encapsulation using appropriate carrier vehicles is highlighted as an effective technique for their stabilization and protection. The aim of this study is to microencapsulate dandelion leaf extract using spray drying and different carrier materials for the first time. Experimental approach. In spray drying, low inlet temperature of 130 °C was employed to preserve sensitive dandelion polyphenols, while guar gum, gum arabic, inulin, maltodextrin, pectin and alginate were used as carriers. The influence of different carriers and their content on physicochemical, morphological and colour properties, polyphenolic content and encapsulation efficiency of polyphenols in dandelion powders was examined. Specific polyphenols were determined using HPLC-PAD analysis. Their release profiles and antioxidant capacity in simulated gastrointestinal conditions were also evaluated. Results and conclusions. Compared to plain dandelion powder, carrier-containing dandelion powders have favourably increased solubility, enhanced flow and cohesive properties, reduced particle size and prolonged release of polyphenols under simulated gastrointestinal conditions. Powders were characterized by low moisture content (~2–8 %) and high solubility (~92–97 %). Chicoric acid was the most abundant compound in dandelion powders. Pectin-dandelion powder showed to be the most effective for microencapsulation of polyphenols, especially for chicoric acid entrapment (74.4 %). Alginate-dandelion powder enabled the slowest gradual release of polyphenols. Novelty and scientif

Willow gentian as a source of bitter compounds is traditionally used for digestive disorders. Gentiana root extract was spray dried using five different carriers (maltodextrin, whey protein, pectin, starch, gelatine) at various concentrations. Powders were characterized in terms of physical properties and encapsulation efficiency of bioactive compounds. The moisture content of all powders was between 1.78 and 3.46 %, and bulk density from 0.23 to 0.32 g/mL. Powders produced with maltodextrin and whey protein provided the highest yield (around 75 and 70 %, respectively) and the lowest hygroscopicity (6 and 7%, respectively). Gelatin and pectin provided powders with the highest encapsulation efficiency of total phenolic as well as the individual compounds. The stability of encapsulated bioactive compounds was studied after 6 months, and the most stable in all samples were gentiopicrin and sweroside with their content decreased by 10 % only. This study has shown that spray drying of gentian root extract produces powders with good physical properties and encapsulation of bioactives.

Rosa canina pseudo-fruit is rich in bioactive substances, such are carotenoids, ascorbic acid, polyphenols, fatty acids and minerals. Because of its diuretic, anti-inflammatory, anti-allergic and antioxidant properties it is frequently employed in traditional medicine. However, in order to protect mentioned bioactive compounds and to improve its bioavailability and controlled release, numerous encapsulation methods have been developed. Thus, R. canina ethanol extract obtained using percolation at ambient temperature (25°C), was encapsulated into Lipoid G liposomes produced in thin film procedure. Total polyphenol and flavonoid contents, as well as antioxidant potential of the extract and extract loaded liposomes were determined. Encapsulation efficiency, particle size, polydispersity index and zeta potential of the liposomes with extract were monitoring during 30 days. Total polyphenol and flavonoid contents of the extract were 103.8±1.9 mg of gallic acid equivalents/g of the extract and 64.2±2.4 mg of catechin equivalents/g of the extract, respectively; antioxidant potential of the extract was 15.3±2.1 mg of Trolox equivalents/g of the extract (ABTS assay) and 1.07±0.01 mg/mL of the extract (DPPH assay). Total polyphenol and flavonoid contents of the extract loaded liposomes were 0.316±0.023 mg of gallic acid equivalents/mg of lipids and 0.219±0.009 mg of catechin equivalents/mg of lipids, respectively; antioxidant potential of the sample was 0.134±0.004 mg of Trolox equivalents/mg of lipids (ABTS assay) and 270.6±10.5 mg/mL of liposomal suspension (DPPH assay). Encapsulation efficiency was the same during monitoring period and it was amounted 46.6±3.4%. Particle size and polydispersity index of the liposomes with extract were increased from 618.2±10.9 to 1698.0±104.2 nm and from 0.441±0.007 to 0.589±0.011, respectively, during 30 days. On the other hand, zeta potential of the extract loaded liposomes was decreased from -10.24±0.95 to -7.21±0.77 mV. R. canina extra

Polyphenols, as secondary metabolites from plants, are used as food complements or ingredients within the pharmaceutical or cosmetic formulations. However, their use is rather limited, due to their low bioavailability, integrity, permeability, and solubility. Namely, polyphenols’ sensitivity to environmental factors during food processing, distribution, or storage, or in the gastrointestinal tract, also limit their activity and the potential health benefits. Thus, the encapsulation of polyphenol extracts represents an appropriate way to overcome the mentioned disadvantages. Thymus serpyllum L. ethanol extract obtained in heat-assisted extraction (80°C), rich in polyphenol compounds, was encapsulated into liposomes produced using phospholipids and proliposome method. Total polyphenol content in extract and encapsulation efficiency were determined using the Folin-Ciocalteu procedure. Particle size, polydispersity index, and zeta potential of empty and extract loaded liposomes were measured during 28 days using photon correlation spectroscopy. Total polyphenol content of the extract was amounted to 2.08±0.14 mg of gallic acid equivalents/mL, whereas encapsulation efficiency was 89.4±0.8%. During the 28-days stability study, the particle size of empty liposomes varied between 420.6±4.3 and 581.6±3.4 nm with polydispersity index from 0.109±0.067 to 0.295±0.009, while the size of extract loaded liposomes was between 278.7±1.5 and 456.4±9.3 nm with polydispersity index 0.179±0.094 to 0.284±0.005. Zeta potential of empty liposomes varied from -17.1±0.2 to -27.3±0.5 mV, whereas the zeta potential of extract loaded liposomes was between -13.6±0.3 and -25.4±1.4 mV. The aim of this study is to provide evidence for food manufacturers and food scientists to make broader use of T. serpyllum loaded liposomes that can add value and improve the quality of existing food, pharmaceutical and cosmetic products.

Figure S1. The spectrum of folic acid; Figure S2. The spectrum of histidine; Figure S3. The spectrum of phospholipon 90 G; Figure S4. The spectrum of cholesterol; Figure S5. The spectrum of SPAN 20

Lignin nano/microparticles have recently attracted growing interest for various value-additive applications of lignin, especially encapsulation. In this study, in order to establish a highly efficient and highly productive preparation process to effectively utilize technical lignin, a brand-new, slow and exhaustive solution evaporation process following a simple, self-assembly principle was developed using industrial softwood kraft lignin (SKL) from a starting acetone-water (80/20, v/v) solution to recover 100% of the lignin as homogeneous and well-shaped microspheres. The prepared microspheres had a typical average diameter of 0.81 ± 0.15 μm and were hollow with very thin shells (of nanoscale thickness). Based on this developed technique, encapsulation of urea by these lignin microspheres was directly achieved using the same process as hollow lignin microspheres with urea attached to the outside and entrapped inside of the wall. Two distinct urea release rates were observed for the urea-encapsulated microspheres: a fast release of the urea outside the shell wall and a slow (controlled) release of the urea inside the shell wall. The encapsulation efficiency was as high as 46% of the trapped urea as encapsulated inside the lignin microspheres. The slow and exhaustive solution evaporation procedure reported here is a simple and straightforward method for the valorization of industrial kraft lignin as hollow microspheres with controllable, homogeneous and desired morphologies, and especially for the direct preparation of lignin-based encapsulating fertilizers for controlled release., QC 20191106. QC 20200109

[EN] Carvacrol has been encapsulated in polyvinyl alcohol (PVA) matrices by electrospinning and casting. Aqueous solutions containing 15% PVA and 15% carvacrol with respect to polymer have been used, containing or not Tween 85 at 0.3 g/100 g carvacrol. Electrospun mats exhibited beads and thin fibres which became thinner and interrupted when carvacrol was present and retained up to 83% of this compound. The encapsulation efficiency in the electrospun mats decreased in the presence of surfactant, reaching values similar to those of casting (75-77%). The electrospun, surfactant free material was practically amorphous with 40% of the total carvacrol non-thermally releasable. In contrast, when surfactant was present and in cast material, with 40% crystallinity, the strongly bonded carvacrol ratio decreased. Specific PVA - phenolic hydroxyl interactions played an important role in the degree of carvacrol retention in the matrices, which depended on surfactant's presence and processing method

Thymol and the corresponding brominated derivatives constitute important biological active molecules as antibacterial, antioxidant, antifungal, and antiparasitic agents. However, their application is often limited, because their pronounced fragrance, their poor solubility in water, and their high volatility. The encapsulation of different thymol derivatives into biocompatible lignin-microcapsules is presented as a synergy-delivering remedy. The adoption of lignosulfonate as an encapsulating material possessing relevant antioxidant activity, as well as general biocompatibility allows for the development of new materials that are suitable for the application in various fields, especially cosmesis. To this purpose, lignin microcapsules containing thymol, 4-bromothymol, 2,4-dibromothymol, and the corresponding O-methylated derivatives have been efficiently prepared through a sustainable ultrasonication procedure. Actives could be efficiently encapsulated with efficiencies of up to 50%. To evaluate the applicability of such systems for topical purposes, controlled release experiments have been performed in acetate buffer at pH 5.4, to simulate skin pH: all of the capsules show a slow release of actives, which is strongly determined by their inherent lipophilicity.

In this study, development of folic acid-loaded liposomes using a basic amino acid, histidine as a solubilizing agent for folic acid was presented, which tackled the poor solubility of this vitamin. The effect of the liposomal membrane modifiers, cholesterol and SPAN 20 on the characteristics of the final formulations was examined. Liposomes prepared from a commercially available purified soybean lecithin (Phospholipon 90G) by proliposome method were between 503 and 877 nm in average diameter, where cholesterol induced enlargement and SPAN.20 reduction of vesicles. High encapsulation efficiency of 84% and drug loading of 0.123 mg g(-1) were achieved, irrespective to the composition. According to AFM images, folic acid-loaded liposomes of a fraction with a nano size were flattened compared to globular empty liposomes. FTIR analysis revealed possible interactions between phospholipids and histidine, while DSC study suggested interactions between folic acid and lipids during heating. Release study done by a Franz diffusion cell showed prolonged release of folic acid from liposomes and the release rate was determined by folic acid solubility.

Figure S1. The spectrum of folic acid; Figure S2. The spectrum of histidine; Figure S3. The spectrum of phospholipon 90 G; Figure S4. The spectrum of cholesterol; Figure S5. The spectrum of SPAN 20

In this study, development of folic acid-loaded liposomes using a basic amino acid, histidine as a solubilizing agent for folic acid was presented, which tackled the poor solubility of this vitamin. The effect of the liposomal membrane modifiers, cholesterol and SPAN 20 on the characteristics of the final formulations was examined. Liposomes prepared from a commercially available purified soybean lecithin (Phospholipon 90G) by proliposome method were between 503 and 877 nm in average diameter, where cholesterol induced enlargement and SPAN.20 reduction of vesicles. High encapsulation efficiency of 84% and drug loading of 0.123 mg g−1 were achieved, irrespective to the composition. According to AFM images, folic acid-loaded liposomes of a fraction with a nano size were flattened compared to globular empty liposomes. FTIR analysis revealed possible interactions between phospholipids and histidine, while DSC study suggested interactions between folic acid and lipids during heating. Release study done by a Franz diffusion cell showed prolonged release of folic acid from liposomes and the release rate was determined by folic acid solubility.

Zein is a non-polar protein that has a high content of proline and leucine, it can be easily obtained from corn grains and by its composition can form a protein matrix of nanoparticles to encapsulate polar dyes. From decolorized USP zein, nanoparticles were synthesized by the liquid-liquid dispersion method. The synthesis was carried out in 20% ethanol and pH 4, conditions that allow the highest stability of the system. A homogeneous suspension with a particle size of 282,1 nm and a polydispersity of 0.127 corresponding to a surface area of ​​18.82 m2 / g was obtained; it was evidenced that the particles have a spherical shape and do not present porosity. The nanoparticles thus obtained were used to encapsulate anthocyanins extracted from the mortiño fruit (Vaccinium floribundum Kunth) using the methods of adsorption and incorporation. It was determined that the adsorption method allows to load 338.24 mg of cyanidin-3-glucoside, equivalent to 172.92 g of anthocyanins, per 100 g of nanoparticles, compared with the incorporation method that allowed to encapsulate 72.74 mg of cyanidin-3-glucoside, equivalent to 37.19 g of anthocyanins, per 100 g of nanoparticles. The values ​​of the encapsulation efficiency and load capacity allow to establish that the zein has a high potential encapsulant, La zeína es una proteína no polar que tiene un elevado contenido de prolina y leucina, se puede obtener fácilmente de los granos de maíz y por su composición puede formar una matriz proteica de nanopartículas para encapsular colorantes polares. A partir de zeína USP decolorada, se sintetizaron nanopartículas por el método de dispersión líquido – líquido. La síntesis se llevó a cabo en etanol al 20% y a pH 4, condiciones que permiten la más alta estabilidad del sistema. Se obtuvo una suspensión homogénea con un tamaño de partícula de 282,1 nm y una polidispersión de 0,127 correspondiente a un área superficial de 18,82 m2/g; se evidenció que las partículas tienen forma esférica y no presentan porosidad. Las nanopartículas asi obtenidas se utilizaron para encapsular antocianinas extraídas del fruto de mortiño (Vaccinium floribundum Kunth) utilizando los métodos de adsorción e incorporación. Se determinó que el método de adsorción permite cargar 338,24 mg de cianidina-3-glucósido, equivalente a 172,92 g de antocianinas, por cada 100 g de nanopartículas, comparado con el método de incorporación que permitió encapsular 72,74 mg de cianidina-3-glucósido, equivalente a 37,19 g de antocianinas, por cada 100 g de nanopartículas. Los valores de la eficiencia de encapsulación y capacidad de carga de 32,83±2,84% y 141,38±5,41% respectivamente, permiten establecer que la zeína tiene un alto potencial encapsulante.

The aim of this study was to improve the stability and antioxidant activity of yarrow phenolic compounds upon an in vitro simulated gastrointestinal digestion. Therefore, two types of caseins-based delivery systems, sodium caseinate stabilized nanoemulsions (NEs) and glucono delta-lactone acidified milk gels (MGs), were formulated containing an ultrasound-assisted yarrow extract (YE) at two concentrations (1 and 2.5 mg/mL). Formulations with 1 mg/mL of YE were chosen based on their higher encapsulation efficiency to perform the in vitro digestion experiments. After digestion, YE-loaded NEs only partially protected phenolic compounds from degradation; meanwhile the phenolic composition of YE including in MGs after digestion was quite similar to undigested YE. Moreover, the antioxidant activity of MGs after digestion was higher than NEs digested samples, which confirms the higher protection of YE phenolic compound by the milk gels systems. This research demonstrated the potential use of acidified MGs as carriers to improve the stability and antioxidant activity of yarrow phenolic compounds. Therefore, these matrices could be employed to develop new dairy products enriched with phenolic compounds.

Drug-loaded poly (vinyl alcohol) (PVA)-based microparticles have been synthetized by using membrane emulsification and chemical cross-linking. The encapsulation of two water-soluble molecules, catechol (CA) and diclofenac sodium (DS), has been considered as case studies. PVA hydrogels have been recognized as promising biomaterials and suitable candidates for drug delivery. However, the encapsulation of hydrophilic, low molecular weight drugs in particulate materials is currently an ambitious goal. The purpose of this work was to develop high-drug loading systems for hydrophilic molecule delivery based on uniformly distributed particulate carriers. Membrane emulsification has been used as advanced manufacturing method to design drug-loaded PVA microparticles with target properties in terms of particle size, particle size distribution, structure and functional activity. A special emphasis is laid on the important factors that contribute to tune the structured properties of microparticles, encapsulation efficiency/drug loading and drug delivery. In particular, the influence of emulsification method (membrane and homogenizing approaches), phase compositions (PVA concentration, drug concentration, physicochemical properties of drug), cross-linking reaction conditions (cross-linking agent concentration, acidic media) has been studied. Finally, the potential of PVA-based microparticles as drug delivery carriers as well as their in vitro cytotoxicity have been evaluated.

This study investigated the oxidative stability and physical properties of low-fat mayonnaise fortified with electrosprayed zein capsules loaded with fish oil. A high encapsulation efficiency (EE) (83 ± 1%) was achieved in the encapsulates and semi-spherical capsules with rough surface and mean diameter of 2.4 ± 0.7 μm were obtained. The amount of primary oxidation products of the zein capsules did not increase over the storage, even though the initial content was higher compared to neat fish oil. Cryo-SEM images revealed that the capsules remained intact when they were incorporated into a water-based food matrix like mayonnaise. This explained the lower content of hydroperoxides at the end of the storage for the capsule-enriched mayonnaise (Mayo-C) when compared to mayonnaise enriched with neat fish oil (Mayo-F) (2 meq/kg oil vs. 6 meq/kg oil, respectively). Even though, volatile compounds from the secondary oxidation of omega-3, such as 2-ethylfuran and 1-penten-3-one were found in higher amounts in Mayo-F, a higher overall increase in all other secondary oxidation products was observed in Mayo-C. This increase was attributed to the formation of oxidation volatile compounds from the zein material, together with the oxidation of un-encapsulated fish oil droplets. Moreover, Mayo-C presented higher viscosity and droplet size than Mayo-F, which also increased during storage, although no further alterations of the emulsion like creaming were observed. Overall, these findings indicate the benefits of using zein as hydrophobic shell material for the development of omega-3 loaded-electrosprayed capsules intended to the enrichment of water-based food matrices when compared to the use of hydrophilic wall materials.

[EN] The encapsulation of eugenol (E) by spray-drying using whey protein (WP) or soy lecithin (LE) and maltodextrin in combination with oleic acid (OA) and chitosan (CH) was analysed in order to obtain antioxidant and antimicrobial powders for food applications. Formulations with only WP or LE showed higher encapsulation efficiencies (EE) (95¿98%) and antibacterial effect against E. coli and L. innocua due to their greater E load. Incorporation of OA or CH promoted lower EE, which negatively affected the antimicrobial and antioxidant activities of the powders. Furthermore, the addition of CH implied less thermal protection against the E losses. The eugenol release was not notably affected by pH or polarity of the food simulant, but the release rate significantly decreased when incorporating OA and CH. The E-LE formulations better retained the eugenol than E-WP powders when heated above 200¿°C, this being relevant for the powder inclusion in thermally treated products.

Bioactive peptides carry antioxidative activity and have the potential to be used as additives in food formulation. When incorporated, major instability of peptides is imposed within heterogeneous products, as well as the loss of biological activity in the gastrointestinal system before absorption into the bloodstream and manifestation of biological activity at the target site in the body. A good solution as a controlled release system is liposomes – particles made out of phospholipids, natural molecules and a building block of the cell membrane. Therefore, the aim of this study was to prepare new systems for the encapsulation and controlled release of soybean antioxidant peptides. Liposome preparation was performed by forming a uniform thin film of phospholipon 90-G and hydrating it with an aqueous solution of soy protein concentrate hydrolyzate prepared by a two-step enzymatic process. The last step of liposome preparation was ultrasonic treatment. The size distribution, surface charge, degree of encapsulation and stability of multilamellar liposomes were characterized. A thin film method provided a satisfying percentage of encapsulation of soybean antioxidant peptides (19%). The ultrasonic homogenizer proved to be three times better than the ultrasonic bath while reducing the size of the particles. The antioxidant activity was tested by neultralization of the ABTS • + radical cation method and by Fe2+ ion chelation method. The test have shown that encapsulation of the peptide activity was partially retained. In the simulated gastrointestinal system, diffusion experiments have shown that liposomes slow down the release of antioxidant peptides. The presented results represent important information for the specific application of liposomes with encapsulated soybean peptides in functional food products.

The aim of this study was to investigate the influence of end group of poly(lactic-co-glycolic acid) (PLGA) on the drug loading and release behavior of electrospray-generated PLGA microspheres. To this end, doxycycline hyclate (DOX) was selected as a model drug, and PLGA (molecular weight: 17 and 44 kDa) with either an acid or ester end group were electrosprayed with DOX. The processing parameters were optimized to obtain microspheres comparable in size. Drug loading efficiency and release profile were determined by the high-performance liquid chromatography-ultraviolet detection (HPLC-UV) method. PLGA polymers or drug-loaded microspheres were characterized before and after exposure to phosphate buffer saline at 37 °C regarding the wettability of polymers, pH changes of the buffer, molecular weight of PLGA and morphology of the microspheres. The acid end group of PLGA microspheres brought about lower encapsulation efficiency and faster DOX release rate in our study, indicating that different hydrophilicity of polymer and degradation speed were the main reasons causing a difference in encapsulation efficiency and release profile. In addition, DOX released from the PLGA microspheres was active by showing antibacterial effects against Porphyromonas gingivalis as measured using a zone of inhibition test, and varying the end groups showed no impact on the antibacterial efficacy. This study demonstrated that the end group of PLGA can be used as a new tool to regulate drug encapsulation efficiency and release rate to meet different clinical drug delivery requirements.

In this study, we established a procedure based on the microencapsulation vesicle (MCV) method for preparing surface-modified liposomes, using polyethylene glycol (PEG) and a site-directed ligand, with high entrapment efficiency of cytochrome c (Cyt c). For preparing a water-in-oil (W/O) emulsion, egg phosphatidylcholine and cholesterol were dissolved in organic solvents (O phase) and emulsified by sonication with aqueous solution of Cyt c (W-1). Although the dispersion stability of the W-1/O emulsion was low when n-hexane was used to dissolve the lipids in the O phase, it was substantially improved by using mixed solvents consisting of n-hexane and other organic solvents, such as ethanol and dichloromethane (DCM). The W-1/O emulsion was then added to another water phase (W-2) to prepare the W-1/O/W-2 emulsion. PEG- and/or ligand-modified lipids were introduced into the W-2 phase as external emulsifiers not only for stabilizing the W-1/O/W-2 emulsion but also for modifying the surface of liposomes obtained later. After solvent evaporation and extrusion for downsizing the liposomes, approximately 50% of Cyt c was encapsulated in the liposomes when the mixed solvent consisting of n-hexane and DCM at a volume ratio of 75/25 was used in the O phase. Finally, the fluorescence-labeled liposomes, with a peptide ligand having affinity to the vasculature in adipose tissue, were prepared by the MCV method and intravenously injected into mice. Confocal microscopy showed the substantial accumulation of these liposomes in the adipose tissue vessels. Taken together, the MCV technique, along with solvent optimization, could be useful for generating surface-modified liposomes with high drug entrapment efficiency for targeted delivery.

[EN] Potential factors leading to surface oil were investigated by analyzing the impact of emulsion properties, atomization and drying conditions separately. An increased oil load, droplet size and in particular the size of droplet aggregates led to significant more surface oil. Increasing the viscosity, inlet temperature and relative humidity resulted in larger particles with a higher encapsulation efficiency. The results indicate that the probability of oil droplets being in contact with the particle surface determines the amount of surface oil. Oil diffusion towards the surface was excluded due to the short residence times and high viscosities.

Poly(lactide-co-glycolide) (PLGA) microspheres are efficient delivery systems for controlled release of low molecular weight drugs as well as therapeutic macromolecules. The most common microencapsulation methods are based on emulsification procedures, in which emulsified droplets of polymer and drug solidify into microspheres when the solvent is extracted from the polymeric phase. Although high encapsulation efficiencies have been reported for hydrophobic small molecules, encapsulation of hydrophilic and/or amphiphilic small molecules is challenging due to the partitioning of drug from the polymeric phase into the external phase before solidification of the particles. This review addresses formulation-related aspects for efficient encapsulation of small hydrophilic/amphiphilic molecules into PLGA microspheres using conventional emulsification methods (e.g., oil/water, water/oil/water, solid/oil/water, water/oil/oil) and highlights novel emulsification technologies such as microfluidics, membrane emulsification and other techniques including spray drying and inkjet printing. Collectively, these novel microencapsulation technologies afford production of this type of drug loaded microspheres in a robust and well controlled manner.

Encapsulation of nonsteroidal or non-steroidal anti-inflammatory drugs (NSAID) in nanocarrier systems aims to enhance bioavailability and to decrease toxicity of these drugs and thus improve the efficacy of treatments. With this aim two types of nanoparticles were prepared and compared: lipid nanoparticles, made of cetyl palmitate and Miglyol 812 which were uncoated or coated with chitosan; or polymeric nanoparticles, made of poly (DL-lactic-co-glycolic acid) (PLGA) for which different emulsion stabilizers were also tested (poly (vinyl alcohol) (PVA), and Pluronic F68). Nanoparticles were characterized for drug content and for particle size, charge and morphology. The lipid matrix was analyzed regarding its crystallinity by differential scanning calorimetry (DSC). The size of the nanoparticles was measured by dynamic light scattering (DLS) which indicated a unimodal particle size distribution in all systems. Nanoparticles' stability was confirmed by their highly negative surface charge in the case of polymeric and uncoated lipid nanoparticles, as analyzed by zeta potential measurements using electrophoretic light scattering (ELS). Lipid chitosan coated nanoparticles have also shown to be stable presenting highly positive surface charge. Results have further demonstrated that indomethacin is highly encapsulated regardless the type of particles. Morphological analysis by scanning electron microscopy has shown that the nanoparticles were smooth and spherical. The results gathered within the current study point to the conclusion that the proposed formulations provide nanoparticles of satisfactory quality to encapsulate indomethacin, which might be used to improve bioavailability of other NSAID in the treatment of inflammation.

The aim of the present study was to investigate the effect of wall materials composition on physicochemical char- acteristics of fish oil microcapsules produced by spray drying (180 °C). Four different combination of coating materials (fish gelatin, chitosan, combination of gelatin and chitosan, and a mixture of microbial transglutaminase (MTGase) with malto- dextrin) were applied to two different fish oils to produce 40 % solid emulsions. Scanning electron microscopy and extraction of surface and encapsulated oils revealed that fish gelatin provided the highest preserving effect on the covering fish oil. Meantime, addition of MTGase to gelatin could also increase this ability and reveled less surface oil than chitosan treatment (2.63 and 2.80 % versus 4.66 and 5.23 %, respec- tively; P <0.05). Mixture of gelatin and maltodextrin with MTGase as wall material led to the highest encapsulation efficiency, being selected as the best microencapsulation con- dition; meantime, application of chitosan with maltodextrin provided the worse encapsulation efficiency ( P <0.05). All indices of powders (encapsulation efficiency, surface mor- phology, and particle size) showed that powders prepared from gelatin and gelatin with MTGase increased the encapsu- lation efficiency and would increase the stability of microcap- sule powders

This work describes the encapsulation of a small, hydrophilic molecule (clonidine) into a PLGA matrix to provide sustained release over more than one month after intra-articular administration. The microparticles were prepared using a double emulsion (w(1)/o/w(2)) method followed by evaporation of the organic solvent. To optimize the efficiency of encapsulation and the mean size of the microparticles, which was targeted around 30μm, the following parameters were modulated: the viscosity and the volume of the organic phase, the molecular weight of the polymer, the volume of the internal and external aqueous phases, the drug loading, the concentration of surfactant, and the stirring parameters. Blends of polymers characterized by different molecular weights (34000-96000Da) as well as copolymers of PLGA-PEG were used to enhance the entrapment of the drug. The pH of the aqueous phases was adjusted to obtain suitable encapsulation efficiency. Characterization was made of the physico-chemical properties of the microparticles, such as their crystallinity (DSC and PXRD) and microstructure (SEM). When performing in vitro dissolution studies, controlled release for up to approximately 30days was achieved with several of the formulations developed. Diffusion was found to be the dominant drug release mechanism at early time points., JOURNAL ARTICLE, SCOPUS: ar.j, info:eu-repo/semantics/published

Stirred cell membrane emulsification was used to create double water-in-oil-in-water emulsions at the dispersed phase flux of up to 3200 L m(-2) h(-1). The oil phase was unrefined pumpkin seed oil or sunflower oil containing 30% by volume of internal water phase and the external water phase was 2% Tween 20 (polyoxyethylene sorbitan monolaurate) or 2% Pluronic F-68 (polyoxyethylene-polyoxypropylen copolymer). Using microengineered nickel membranes with pore sizes between 15 and 40 mu m, median drop sizes of double emulsion droplets were in the range between 100 and 430 mu m, depending mainly on the shear at the membrane surface and dispersed phase injection rate. In most cases the drops were very uniform, with span (i.e. 90% drop size minus 10% drop size divided by median size) values of around 0.5. This data is similar to what was obtained previously for simple O/W emulsions of the same materials. Hence, the internal water phase, and internal surfactant, 5% PGPR (polyglycerol polyricinoleate), did not adversely influence the emulsification process. A marker material, copper sulfate, was added to the internal water phase and the release of copper was monitored with respect to time. For both lipid systems, at the larger droplet size, there was a significant period of no copper release, followed by almost linear release with time. This initial period was absent when the drop size was close to 100 mu m. The initial entrapment efficiency of the copper, in all experiments, was higher than 94%. (C) 2011 Elsevier B. V. All rights reserved.

Tato diplomová práce se zabývá studiem inkorporace nízko a vysokomolekulárních látek do liposomálních systémů. Cílem práce bylo stanovit enkapsulační účinnost (EE) vybraných látek a vliv jednotlivých komponent liposomálního systému na EE. Liposomy byly připraveny z dipalmitoylfosfatidylcholinu, stabilizovány byly přídavkem cholesterolu a přídavkem kyseliny fosfatidové získaly záporný náboj. Stealth vlastnosti získaly navázáním polyethylenglykolu a přídavkem trimethylchitosanu byl umožněn vstup liposomů do krevního řečiště paracelulární cestou. K inkorporaci do liposomů byl použit vitamín C a enzym bromelain. Ke zjištění enkapsulační účinnosti liposomů připravených kombinací jednotlivých složek byla použita metoda UV-VIS spektrofotometrie. Bylo zjištěno, že vitamín C a enzym lze inkorporovat do liposomů, kdy enzym vykazuje vyšší EE. Dále bylo zjištěno, že největší vliv na EE má kyselina fosfatidová a trimethylchitosan, který zvyšuje EE vitamínu C a naopak snižuje EE enzymu., This master´s thesis deals with the study of the incorporation of low and high molecular weight substances into liposomal systems. The aim of the work was to determine the encapsulation efficiency (EE) of the active substance and the influence of individual components of the liposomal system on EE. Liposomes were prepared from dipalmitoylphosphatidylcholine. They were stabilized by cholesteroland and phosphatidic acid was added to give a negative charge. Stealth properties gain the binding of polyethylene glycol and other trimethyl chitosan we enabled the entry of liposomes into the bloodstream by the paracellular pathway. Vitamin C and the enzyme bromelain were used for incorporation into liposomes. UV-VIS spectrophotometry was used to determine the encapsulation efficiency of liposomes prepared by combining the individual components. It has been suggested that vitamin C and the enzyme can be incorporated into liposomes, but an enzyme with a higher EE. Furthermore, phosphatidic acid and trimethyl chitosan have been found to affect EE, which increases the EE of vitamin C and decreases the EE of the enzyme.

Tato bakalářská práce se zabývá studiem enkapsulační účinnosti hydrofilní látky a jejím uvolňováním z vodného středu v závislosti na odlišném složení komponent jednotlivých lipozomálních systémů. Jako modelové léčivo byla vybrána hydrofilní fluorescenční sonda zvaná pyranin. Cílem bylo připravit lipozomy, které by byly z hlediska jejich vlastností vhodné pro inhalační podávání a které by zajistily pasivní cílení s prodlouženou dobou uvolňování bez vyvolání vedlejších účinků na organismus. Podařilo se nám vytvořit standardní operační postup pro inkorporaci hydrofilních látek. Byly připraveny lipozomální systémy skládající se z přídavků různých komponent, jako je cholesterol, kyselina fosfatidová, polyethylenglykol navázaný na fosfatidylethanolamin a trimethylchitosan. Dále se nám podařilo charakterizovat jednotlivé lipozomální systémy z hlediska velikosti, stability a enkapsulační účinnosti, což jsou důležité fyzikálně-chemické vlastnosti pro další aplikační potenciál., This bachelor thesis deals with the study of the encapsulation efficiency of hydrophilic drugs and their releasing from the aqueous core depending on the different composition of the components of individual liposomal systems. The hydrophilic fluorescent probe called pyranine was chosen as a model drug. The aim was to prepare liposomes which would be suitable for inhalation administration in terms of their properties. These liposomes would provide passive targeting with prolonged release time without causing negative side effects on the organism. We have succeeded in developing a standard operating procedure for the incorporation of hydrophilic drugs. Liposomal systems have been prepared consisting of the addition of various components as cholesterol, phosphatidic acid, pegylated phosphatidylethanolamine and trimethylchitosan. Furthermore, we were able to characterize the individual liposomal systems in terms of size, stability and encapsulation efficiency which are important physicochemical properties for further application potential.

Tato diplomová práce se zabývá studiem enkapsulační účinnosti antibiotika doxycyklinu v lipozomálních systémech s odlišným složením komponent. Pojednává i o kinetice uvolňování enkapsulovaného léčiva z těchto nosičových systémů. Lipozomální systémy pro léčbu lokálních plicních onemocnění byly vybrány na základě vhodných fyzikálně chemických vlastností. Jako mikroorganismus, který modeluje lokální plicní onemocnění, plicní pneumonii, byla vybrána bakterie Staphylococcus aureus. Doxycyklin byl zvolen jako antibiotikum ideální pro léčbu stafylokokové infekce. Cílem bylo optimalizovat složení lipozomů tak, aby měly lipozomální systémy aplikační potenciál pro inhalační podávání léčiv. Byly připraveny dva vhodné lipozomální systémy skládající se z přídavků cholesterolu a kyseliny fosfatidové. Podařilo se nám určit koncentraci léčiva pro enkapsulaci, která měla dostatečnou antimikrobiální účinnost pro léčbu lokálního plicního onemocnění. Ke stanovení vedlejších účinků zvolených lipozomálních systémů byly využity cytotoxické testy. Dále byly jednotlivé lipozomální systémy charakterizované z hlediska velikosti, zeta potenciálu a kinetické stability, což jsou další důležité vlastnosti ovlivňující jejich budoucí aplikační potenciál., This diploma thesis deals with the study of the encapsulation efficiency of the antibiotic doxycycline encapsulated in the individual liposomal systems depending on different composition of the components. We also discussed the kinetics of the encapsulated drug releasing from the carrier systems. The liposomal systems for the treatment of local lung diseases were selected due to their suitable physicochemical properties. The bacterium called Staphylococcus aureus was chosen as a model of the local lung disease, pulmonary pneumonia. Doxycycline was chosen as the antibiotic ideal for the treatment of staphylococcal infection. The aim of the diploma thesis was to optimize the composition of liposomes which would have application potential for the inhalation administration of drugs. Two suitable liposomal systems have been prepared consisting of the addition of various components as cholesterol and phosphatidic acid. We have succeeded in determination of the drug concentration for the encapsulation which had sufficient antimicrobial efficacy to treat the local lung disease. The cytotoxic tests were used to determine the side effects of selected liposomal systems. Furthermore, the individual liposomal systems were characterized in terms of size, zeta potential and kinetic stability which are other important properties effecting their future application potential.

Tato diplomová práce se zabývá studiem enkapsulační účinnosti antibiotika doxycyklinu v lipozomálních systémech s odlišným složením komponent. Pojednává i o kinetice uvolňování enkapsulovaného léčiva z těchto nosičových systémů. Lipozomální systémy pro léčbu lokálních plicních onemocnění byly vybrány na základě vhodných fyzikálně chemických vlastností. Jako mikroorganismus, který modeluje lokální plicní onemocnění, plicní pneumonii, byla vybrána bakterie Staphylococcus aureus. Doxycyklin byl zvolen jako antibiotikum ideální pro léčbu stafylokokové infekce. Cílem bylo optimalizovat složení lipozomů tak, aby měly lipozomální systémy aplikační potenciál pro inhalační podávání léčiv. Byly připraveny dva vhodné lipozomální systémy skládající se z přídavků cholesterolu a kyseliny fosfatidové. Podařilo se nám určit koncentraci léčiva pro enkapsulaci, která měla dostatečnou antimikrobiální účinnost pro léčbu lokálního plicního onemocnění. Ke stanovení vedlejších účinků zvolených lipozomálních systémů byly využity cytotoxické testy. Dále byly jednotlivé lipozomální systémy charakterizované z hlediska velikosti, zeta potenciálu a kinetické stability, což jsou další důležité vlastnosti ovlivňující jejich budoucí aplikační potenciál., This diploma thesis deals with the study of the encapsulation efficiency of the antibiotic doxycycline encapsulated in the individual liposomal systems depending on different composition of the components. We also discussed the kinetics of the encapsulated drug releasing from the carrier systems. The liposomal systems for the treatment of local lung diseases were selected due to their suitable physicochemical properties. The bacterium called Staphylococcus aureus was chosen as a model of the local lung disease, pulmonary pneumonia. Doxycycline was chosen as the antibiotic ideal for the treatment of staphylococcal infection. The aim of the diploma thesis was to optimize the composition of liposomes which would have application potential for the inhalation administration of drugs. Two suitable liposomal systems have been prepared consisting of the addition of various components as cholesterol and phosphatidic acid. We have succeeded in determination of the drug concentration for the encapsulation which had sufficient antimicrobial efficacy to treat the local lung disease. The cytotoxic tests were used to determine the side effects of selected liposomal systems. Furthermore, the individual liposomal systems were characterized in terms of size, zeta potential and kinetic stability which are other important properties effecting their future application potential.

Tato diplomová práce se zabývá charakterizací a přípravou kataniontových vezikulárních systémů a jejich následnou interakcí s ve vodě nerozpustnými vitamíny. Kataniontové vezikulární systémy byly připraveny z dvou různě nabitých povrchově aktivních látek CTAB a SDS za vzniku iontového amfifilního páru. Stabilita vezikul byla zajištěna přidáním cholesterolu spolu s kladně nabitou povrchově aktivní látkou DODAC. Pro následnou solubilizaci do těchto vezikul byl vybrán vitamín A a vitamín E. Další část práce byla zaměřena na stanovení efektivity inkorporace těchto vitamínů do vezikulárních systémů HTMA-DS. Charakterizace těchto systémů byla provedena pomocí měření na UV-VIS spektrometru, DLS a pomocí HPLC s UV-VIS detektorem. Během měření na UV-VIS a HPLC byla stanovena účinnost solubilizace vitamínu A a vitamínu E do vezikul. V obou případech byla stanovena vyšší účinnost u vezikul s inkorporovaným vitamínem A. Vyšší účinnost u obou vitamínů byla stanovena pomocí metody HPLC. Důvodem je pravděpodobně vyšší citlivost metody, práce s tmavým sklem a příprava jednotlivých vzorků do vialek, které byly následně vloženy do přístroje pro jednotlivé dávkování pomocí injektoru. Práce slouží především ke zhodnocení výsledků z hlediska použitelnosti daného vezikulárního systému za účelem uplatnění ve farmaceutických aplikacích jako nosiče nepolárních vitamínů., This thesis deals with the characterization and preparation of catanionic vesicular systems and their interaction with water-insoluble vitamins. Catanionic vesicles systems was prepared from two differently charged sufractants CTAB and SDS in formation ion pair amphiphile. Stability of vesicles was secured by adding cholesterol with positively charged surfactant DODAC. Were selected vitamin A and vitamin E for solubilization into these vesicles. The next part of this work was focused on determining the efficiency of incorporation these vitamins into the HTMA-DS vesicular system. The characterization of these systems was improved by measurement on a UV-VIS spectrometer, DLS and by HPLC with UV-VIS detector. During measurement by UV-VIS and HPLC the efficiency of solubilization of vitamin A and vitamin E into vesicles was determinated. In both cases higher efficiency was determinated for vesicles with incorporated vitamin A. Higher efficiency for both vitamins was determinated by HPLC. The reason is probably the higher sensitivity of the metod, work in labs with dark glass and preparing individuals samples into vials, which were inserted into the device for individual dosing by injector. The work serves primary evaluation results in view of the vesicular system for use in pharmaceutical application like carrier non-polar vitamins.

Tato bakalářská práce se zabývá studiem enkapsulační účinnosti hydrofilní látky a jejím uvolňováním z vodného středu v závislosti na odlišném složení komponent jednotlivých lipozomálních systémů. Jako modelové léčivo byla vybrána hydrofilní fluorescenční sonda zvaná pyranin. Cílem bylo připravit lipozomy, které by byly z hlediska jejich vlastností vhodné pro inhalační podávání a které by zajistily pasivní cílení s prodlouženou dobou uvolňování bez vyvolání vedlejších účinků na organismus. Podařilo se nám vytvořit standardní operační postup pro inkorporaci hydrofilních látek. Byly připraveny lipozomální systémy skládající se z přídavků různých komponent, jako je cholesterol, kyselina fosfatidová, polyethylenglykol navázaný na fosfatidylethanolamin a trimethylchitosan. Dále se nám podařilo charakterizovat jednotlivé lipozomální systémy z hlediska velikosti, stability a enkapsulační účinnosti, což jsou důležité fyzikálně-chemické vlastnosti pro další aplikační potenciál., This bachelor thesis deals with the study of the encapsulation efficiency of hydrophilic drugs and their releasing from the aqueous core depending on the different composition of the components of individual liposomal systems. The hydrophilic fluorescent probe called pyranine was chosen as a model drug. The aim was to prepare liposomes which would be suitable for inhalation administration in terms of their properties. These liposomes would provide passive targeting with prolonged release time without causing negative side effects on the organism. We have succeeded in developing a standard operating procedure for the incorporation of hydrophilic drugs. Liposomal systems have been prepared consisting of the addition of various components as cholesterol, phosphatidic acid, pegylated phosphatidylethanolamine and trimethylchitosan. Furthermore, we were able to characterize the individual liposomal systems in terms of size, stability and encapsulation efficiency which are important physicochemical properties for further application potential.

Tato diplomová práce se zabývá charakterizací a přípravou kataniontových vezikulárních systémů a jejich následnou interakcí s ve vodě nerozpustnými vitamíny. Kataniontové vezikulární systémy byly připraveny z dvou různě nabitých povrchově aktivních látek CTAB a SDS za vzniku iontového amfifilního páru. Stabilita vezikul byla zajištěna přidáním cholesterolu spolu s kladně nabitou povrchově aktivní látkou DODAC. Pro následnou solubilizaci do těchto vezikul byl vybrán vitamín A a vitamín E. Další část práce byla zaměřena na stanovení efektivity inkorporace těchto vitamínů do vezikulárních systémů HTMA-DS. Charakterizace těchto systémů byla provedena pomocí měření na UV-VIS spektrometru, DLS a pomocí HPLC s UV-VIS detektorem. Během měření na UV-VIS a HPLC byla stanovena účinnost solubilizace vitamínu A a vitamínu E do vezikul. V obou případech byla stanovena vyšší účinnost u vezikul s inkorporovaným vitamínem A. Vyšší účinnost u obou vitamínů byla stanovena pomocí metody HPLC. Důvodem je pravděpodobně vyšší citlivost metody, práce s tmavým sklem a příprava jednotlivých vzorků do vialek, které byly následně vloženy do přístroje pro jednotlivé dávkování pomocí injektoru. Práce slouží především ke zhodnocení výsledků z hlediska použitelnosti daného vezikulárního systému za účelem uplatnění ve farmaceutických aplikacích jako nosiče nepolárních vitamínů., This thesis deals with the characterization and preparation of catanionic vesicular systems and their interaction with water-insoluble vitamins. Catanionic vesicles systems was prepared from two differently charged sufractants CTAB and SDS in formation ion pair amphiphile. Stability of vesicles was secured by adding cholesterol with positively charged surfactant DODAC. Were selected vitamin A and vitamin E for solubilization into these vesicles. The next part of this work was focused on determining the efficiency of incorporation these vitamins into the HTMA-DS vesicular system. The characterization of these systems was improved by measurement on a UV-VIS spectrometer, DLS and by HPLC with UV-VIS detector. During measurement by UV-VIS and HPLC the efficiency of solubilization of vitamin A and vitamin E into vesicles was determinated. In both cases higher efficiency was determinated for vesicles with incorporated vitamin A. Higher efficiency for both vitamins was determinated by HPLC. The reason is probably the higher sensitivity of the metod, work in labs with dark glass and preparing individuals samples into vials, which were inserted into the device for individual dosing by injector. The work serves primary evaluation results in view of the vesicular system for use in pharmaceutical application like carrier non-polar vitamins.

Tato diplomová práce se zabývá studiem inkorporace nízko a vysokomolekulárních látek do liposomálních systémů. Cílem práce bylo stanovit enkapsulační účinnost (EE) vybraných látek a vliv jednotlivých komponent liposomálního systému na EE. Liposomy byly připraveny z dipalmitoylfosfatidylcholinu, stabilizovány byly přídavkem cholesterolu a přídavkem kyseliny fosfatidové získaly záporný náboj. Stealth vlastnosti získaly navázáním polyethylenglykolu a přídavkem trimethylchitosanu byl umožněn vstup liposomů do krevního řečiště paracelulární cestou. K inkorporaci do liposomů byl použit vitamín C a enzym bromelain. Ke zjištění enkapsulační účinnosti liposomů připravených kombinací jednotlivých složek byla použita metoda UV-VIS spektrofotometrie. Bylo zjištěno, že vitamín C a enzym lze inkorporovat do liposomů, kdy enzym vykazuje vyšší EE. Dále bylo zjištěno, že největší vliv na EE má kyselina fosfatidová a trimethylchitosan, který zvyšuje EE vitamínu C a naopak snižuje EE enzymu., This master´s thesis deals with the study of the incorporation of low and high molecular weight substances into liposomal systems. The aim of the work was to determine the encapsulation efficiency (EE) of the active substance and the influence of individual components of the liposomal system on EE. Liposomes were prepared from dipalmitoylphosphatidylcholine. They were stabilized by cholesteroland and phosphatidic acid was added to give a negative charge. Stealth properties gain the binding of polyethylene glycol and other trimethyl chitosan we enabled the entry of liposomes into the bloodstream by the paracellular pathway. Vitamin C and the enzyme bromelain were used for incorporation into liposomes. UV-VIS spectrophotometry was used to determine the encapsulation efficiency of liposomes prepared by combining the individual components. It has been suggested that vitamin C and the enzyme can be incorporated into liposomes, but an enzyme with a higher EE. Furthermore, phosphatidic acid and trimethyl chitosan have been found to affect EE, which increases the EE of vitamin C and decreases the EE of the enzyme.

Tato bakalářská práce se zabývá studiem enkapsulační účinnosti hydrofilní látky a jejím uvolňováním z vodného středu v závislosti na odlišném složení komponent jednotlivých lipozomálních systémů. Jako modelové léčivo byla vybrána hydrofilní fluorescenční sonda zvaná pyranin. Cílem bylo připravit lipozomy, které by byly z hlediska jejich vlastností vhodné pro inhalační podávání a které by zajistily pasivní cílení s prodlouženou dobou uvolňování bez vyvolání vedlejších účinků na organismus. Podařilo se nám vytvořit standardní operační postup pro inkorporaci hydrofilních látek. Byly připraveny lipozomální systémy skládající se z přídavků různých komponent, jako je cholesterol, kyselina fosfatidová, polyethylenglykol navázaný na fosfatidylethanolamin a trimethylchitosan. Dále se nám podařilo charakterizovat jednotlivé lipozomální systémy z hlediska velikosti, stability a enkapsulační účinnosti, což jsou důležité fyzikálně-chemické vlastnosti pro další aplikační potenciál., This bachelor thesis deals with the study of the encapsulation efficiency of hydrophilic drugs and their releasing from the aqueous core depending on the different composition of the components of individual liposomal systems. The hydrophilic fluorescent probe called pyranine was chosen as a model drug. The aim was to prepare liposomes which would be suitable for inhalation administration in terms of their properties. These liposomes would provide passive targeting with prolonged release time without causing negative side effects on the organism. We have succeeded in developing a standard operating procedure for the incorporation of hydrophilic drugs. Liposomal systems have been prepared consisting of the addition of various components as cholesterol, phosphatidic acid, pegylated phosphatidylethanolamine and trimethylchitosan. Furthermore, we were able to characterize the individual liposomal systems in terms of size, stability and encapsulation efficiency which are important physicochemical properties for further application potential.

Tato diplomová práce se zabývá studiem enkapsulační účinnosti antibiotika doxycyklinu v lipozomálních systémech s odlišným složením komponent. Pojednává i o kinetice uvolňování enkapsulovaného léčiva z těchto nosičových systémů. Lipozomální systémy pro léčbu lokálních plicních onemocnění byly vybrány na základě vhodných fyzikálně chemických vlastností. Jako mikroorganismus, který modeluje lokální plicní onemocnění, plicní pneumonii, byla vybrána bakterie Staphylococcus aureus. Doxycyklin byl zvolen jako antibiotikum ideální pro léčbu stafylokokové infekce. Cílem bylo optimalizovat složení lipozomů tak, aby měly lipozomální systémy aplikační potenciál pro inhalační podávání léčiv. Byly připraveny dva vhodné lipozomální systémy skládající se z přídavků cholesterolu a kyseliny fosfatidové. Podařilo se nám určit koncentraci léčiva pro enkapsulaci, která měla dostatečnou antimikrobiální účinnost pro léčbu lokálního plicního onemocnění. Ke stanovení vedlejších účinků zvolených lipozomálních systémů byly využity cytotoxické testy. Dále byly jednotlivé lipozomální systémy charakterizované z hlediska velikosti, zeta potenciálu a kinetické stability, což jsou další důležité vlastnosti ovlivňující jejich budoucí aplikační potenciál., This diploma thesis deals with the study of the encapsulation efficiency of the antibiotic doxycycline encapsulated in the individual liposomal systems depending on different composition of the components. We also discussed the kinetics of the encapsulated drug releasing from the carrier systems. The liposomal systems for the treatment of local lung diseases were selected due to their suitable physicochemical properties. The bacterium called Staphylococcus aureus was chosen as a model of the local lung disease, pulmonary pneumonia. Doxycycline was chosen as the antibiotic ideal for the treatment of staphylococcal infection. The aim of the diploma thesis was to optimize the composition of liposomes which would have application potential for the inhalation administration of drugs. Two suitable liposomal systems have been prepared consisting of the addition of various components as cholesterol and phosphatidic acid. We have succeeded in determination of the drug concentration for the encapsulation which had sufficient antimicrobial efficacy to treat the local lung disease. The cytotoxic tests were used to determine the side effects of selected liposomal systems. Furthermore, the individual liposomal systems were characterized in terms of size, zeta potential and kinetic stability which are other important properties effecting their future application potential.

Tato bakalářská práce se zabývá studiem enkapsulační účinnosti hydrofilní látky a jejím uvolňováním z vodného středu v závislosti na odlišném složení komponent jednotlivých lipozomálních systémů. Jako modelové léčivo byla vybrána hydrofilní fluorescenční sonda zvaná pyranin. Cílem bylo připravit lipozomy, které by byly z hlediska jejich vlastností vhodné pro inhalační podávání a které by zajistily pasivní cílení s prodlouženou dobou uvolňování bez vyvolání vedlejších účinků na organismus. Podařilo se nám vytvořit standardní operační postup pro inkorporaci hydrofilních látek. Byly připraveny lipozomální systémy skládající se z přídavků různých komponent, jako je cholesterol, kyselina fosfatidová, polyethylenglykol navázaný na fosfatidylethanolamin a trimethylchitosan. Dále se nám podařilo charakterizovat jednotlivé lipozomální systémy z hlediska velikosti, stability a enkapsulační účinnosti, což jsou důležité fyzikálně-chemické vlastnosti pro další aplikační potenciál., This bachelor thesis deals with the study of the encapsulation efficiency of hydrophilic drugs and their releasing from the aqueous core depending on the different composition of the components of individual liposomal systems. The hydrophilic fluorescent probe called pyranine was chosen as a model drug. The aim was to prepare liposomes which would be suitable for inhalation administration in terms of their properties. These liposomes would provide passive targeting with prolonged release time without causing negative side effects on the organism. We have succeeded in developing a standard operating procedure for the incorporation of hydrophilic drugs. Liposomal systems have been prepared consisting of the addition of various components as cholesterol, phosphatidic acid, pegylated phosphatidylethanolamine and trimethylchitosan. Furthermore, we were able to characterize the individual liposomal systems in terms of size, stability and encapsulation efficiency which are important physicochemical properties for further application potential.

Tato diplomová práce se zabývá charakterizací a přípravou kataniontových vezikulárních systémů a jejich následnou interakcí s ve vodě nerozpustnými vitamíny. Kataniontové vezikulární systémy byly připraveny z dvou různě nabitých povrchově aktivních látek CTAB a SDS za vzniku iontového amfifilního páru. Stabilita vezikul byla zajištěna přidáním cholesterolu spolu s kladně nabitou povrchově aktivní látkou DODAC. Pro následnou solubilizaci do těchto vezikul byl vybrán vitamín A a vitamín E. Další část práce byla zaměřena na stanovení efektivity inkorporace těchto vitamínů do vezikulárních systémů HTMA-DS. Charakterizace těchto systémů byla provedena pomocí měření na UV-VIS spektrometru, DLS a pomocí HPLC s UV-VIS detektorem. Během měření na UV-VIS a HPLC byla stanovena účinnost solubilizace vitamínu A a vitamínu E do vezikul. V obou případech byla stanovena vyšší účinnost u vezikul s inkorporovaným vitamínem A. Vyšší účinnost u obou vitamínů byla stanovena pomocí metody HPLC. Důvodem je pravděpodobně vyšší citlivost metody, práce s tmavým sklem a příprava jednotlivých vzorků do vialek, které byly následně vloženy do přístroje pro jednotlivé dávkování pomocí injektoru. Práce slouží především ke zhodnocení výsledků z hlediska použitelnosti daného vezikulárního systému za účelem uplatnění ve farmaceutických aplikacích jako nosiče nepolárních vitamínů., This thesis deals with the characterization and preparation of catanionic vesicular systems and their interaction with water-insoluble vitamins. Catanionic vesicles systems was prepared from two differently charged sufractants CTAB and SDS in formation ion pair amphiphile. Stability of vesicles was secured by adding cholesterol with positively charged surfactant DODAC. Were selected vitamin A and vitamin E for solubilization into these vesicles. The next part of this work was focused on determining the efficiency of incorporation these vitamins into the HTMA-DS vesicular system. The characterization of these systems was improved by measurement on a UV-VIS spectrometer, DLS and by HPLC with UV-VIS detector. During measurement by UV-VIS and HPLC the efficiency of solubilization of vitamin A and vitamin E into vesicles was determinated. In both cases higher efficiency was determinated for vesicles with incorporated vitamin A. Higher efficiency for both vitamins was determinated by HPLC. The reason is probably the higher sensitivity of the metod, work in labs with dark glass and preparing individuals samples into vials, which were inserted into the device for individual dosing by injector. The work serves primary evaluation results in view of the vesicular system for use in pharmaceutical application like carrier non-polar vitamins.

Tato diplomová práce se zabývá studiem enkapsulační účinnosti antibiotika doxycyklinu v lipozomálních systémech s odlišným složením komponent. Pojednává i o kinetice uvolňování enkapsulovaného léčiva z těchto nosičových systémů. Lipozomální systémy pro léčbu lokálních plicních onemocnění byly vybrány na základě vhodných fyzikálně chemických vlastností. Jako mikroorganismus, který modeluje lokální plicní onemocnění, plicní pneumonii, byla vybrána bakterie Staphylococcus aureus. Doxycyklin byl zvolen jako antibiotikum ideální pro léčbu stafylokokové infekce. Cílem bylo optimalizovat složení lipozomů tak, aby měly lipozomální systémy aplikační potenciál pro inhalační podávání léčiv. Byly připraveny dva vhodné lipozomální systémy skládající se z přídavků cholesterolu a kyseliny fosfatidové. Podařilo se nám určit koncentraci léčiva pro enkapsulaci, která měla dostatečnou antimikrobiální účinnost pro léčbu lokálního plicního onemocnění. Ke stanovení vedlejších účinků zvolených lipozomálních systémů byly využity cytotoxické testy. Dále byly jednotlivé lipozomální systémy charakterizované z hlediska velikosti, zeta potenciálu a kinetické stability, což jsou další důležité vlastnosti ovlivňující jejich budoucí aplikační potenciál., This diploma thesis deals with the study of the encapsulation efficiency of the antibiotic doxycycline encapsulated in the individual liposomal systems depending on different composition of the components. We also discussed the kinetics of the encapsulated drug releasing from the carrier systems. The liposomal systems for the treatment of local lung diseases were selected due to their suitable physicochemical properties. The bacterium called Staphylococcus aureus was chosen as a model of the local lung disease, pulmonary pneumonia. Doxycycline was chosen as the antibiotic ideal for the treatment of staphylococcal infection. The aim of the diploma thesis was to optimize the composition of liposomes which would have application potential for the inhalation administration of drugs. Two suitable liposomal systems have been prepared consisting of the addition of various components as cholesterol and phosphatidic acid. We have succeeded in determination of the drug concentration for the encapsulation which had sufficient antimicrobial efficacy to treat the local lung disease. The cytotoxic tests were used to determine the side effects of selected liposomal systems. Furthermore, the individual liposomal systems were characterized in terms of size, zeta potential and kinetic stability which are other important properties effecting their future application potential.

Tato diplomová práce se zabývá studiem enkapsulační účinnosti antibiotika doxycyklinu v lipozomálních systémech s odlišným složením komponent. Pojednává i o kinetice uvolňování enkapsulovaného léčiva z těchto nosičových systémů. Lipozomální systémy pro léčbu lokálních plicních onemocnění byly vybrány na základě vhodných fyzikálně chemických vlastností. Jako mikroorganismus, který modeluje lokální plicní onemocnění, plicní pneumonii, byla vybrána bakterie Staphylococcus aureus. Doxycyklin byl zvolen jako antibiotikum ideální pro léčbu stafylokokové infekce. Cílem bylo optimalizovat složení lipozomů tak, aby měly lipozomální systémy aplikační potenciál pro inhalační podávání léčiv. Byly připraveny dva vhodné lipozomální systémy skládající se z přídavků cholesterolu a kyseliny fosfatidové. Podařilo se nám určit koncentraci léčiva pro enkapsulaci, která měla dostatečnou antimikrobiální účinnost pro léčbu lokálního plicního onemocnění. Ke stanovení vedlejších účinků zvolených lipozomálních systémů byly využity cytotoxické testy. Dále byly jednotlivé lipozomální systémy charakterizované z hlediska velikosti, zeta potenciálu a kinetické stability, což jsou další důležité vlastnosti ovlivňující jejich budoucí aplikační potenciál., This diploma thesis deals with the study of the encapsulation efficiency of the antibiotic doxycycline encapsulated in the individual liposomal systems depending on different composition of the components. We also discussed the kinetics of the encapsulated drug releasing from the carrier systems. The liposomal systems for the treatment of local lung diseases were selected due to their suitable physicochemical properties. The bacterium called Staphylococcus aureus was chosen as a model of the local lung disease, pulmonary pneumonia. Doxycycline was chosen as the antibiotic ideal for the treatment of staphylococcal infection. The aim of the diploma thesis was to optimize the composition of liposomes which would have application potential for the inhalation administration of drugs. Two suitable liposomal systems have been prepared consisting of the addition of various components as cholesterol and phosphatidic acid. We have succeeded in determination of the drug concentration for the encapsulation which had sufficient antimicrobial efficacy to treat the local lung disease. The cytotoxic tests were used to determine the side effects of selected liposomal systems. Furthermore, the individual liposomal systems were characterized in terms of size, zeta potential and kinetic stability which are other important properties effecting their future application potential.

Tato bakalářská práce se zabývá studiem enkapsulační účinnosti hydrofilní látky a jejím uvolňováním z vodného středu v závislosti na odlišném složení komponent jednotlivých lipozomálních systémů. Jako modelové léčivo byla vybrána hydrofilní fluorescenční sonda zvaná pyranin. Cílem bylo připravit lipozomy, které by byly z hlediska jejich vlastností vhodné pro inhalační podávání a které by zajistily pasivní cílení s prodlouženou dobou uvolňování bez vyvolání vedlejších účinků na organismus. Podařilo se nám vytvořit standardní operační postup pro inkorporaci hydrofilních látek. Byly připraveny lipozomální systémy skládající se z přídavků různých komponent, jako je cholesterol, kyselina fosfatidová, polyethylenglykol navázaný na fosfatidylethanolamin a trimethylchitosan. Dále se nám podařilo charakterizovat jednotlivé lipozomální systémy z hlediska velikosti, stability a enkapsulační účinnosti, což jsou důležité fyzikálně-chemické vlastnosti pro další aplikační potenciál., This bachelor thesis deals with the study of the encapsulation efficiency of hydrophilic drugs and their releasing from the aqueous core depending on the different composition of the components of individual liposomal systems. The hydrophilic fluorescent probe called pyranine was chosen as a model drug. The aim was to prepare liposomes which would be suitable for inhalation administration in terms of their properties. These liposomes would provide passive targeting with prolonged release time without causing negative side effects on the organism. We have succeeded in developing a standard operating procedure for the incorporation of hydrophilic drugs. Liposomal systems have been prepared consisting of the addition of various components as cholesterol, phosphatidic acid, pegylated phosphatidylethanolamine and trimethylchitosan. Furthermore, we were able to characterize the individual liposomal systems in terms of size, stability and encapsulation efficiency which are important physicochemical properties for further application potential.

Tato diplomová práce se zabývá charakterizací a přípravou kataniontových vezikulárních systémů a jejich následnou interakcí s ve vodě nerozpustnými vitamíny. Kataniontové vezikulární systémy byly připraveny z dvou různě nabitých povrchově aktivních látek CTAB a SDS za vzniku iontového amfifilního páru. Stabilita vezikul byla zajištěna přidáním cholesterolu spolu s kladně nabitou povrchově aktivní látkou DODAC. Pro následnou solubilizaci do těchto vezikul byl vybrán vitamín A a vitamín E. Další část práce byla zaměřena na stanovení efektivity inkorporace těchto vitamínů do vezikulárních systémů HTMA-DS. Charakterizace těchto systémů byla provedena pomocí měření na UV-VIS spektrometru, DLS a pomocí HPLC s UV-VIS detektorem. Během měření na UV-VIS a HPLC byla stanovena účinnost solubilizace vitamínu A a vitamínu E do vezikul. V obou případech byla stanovena vyšší účinnost u vezikul s inkorporovaným vitamínem A. Vyšší účinnost u obou vitamínů byla stanovena pomocí metody HPLC. Důvodem je pravděpodobně vyšší citlivost metody, práce s tmavým sklem a příprava jednotlivých vzorků do vialek, které byly následně vloženy do přístroje pro jednotlivé dávkování pomocí injektoru. Práce slouží především ke zhodnocení výsledků z hlediska použitelnosti daného vezikulárního systému za účelem uplatnění ve farmaceutických aplikacích jako nosiče nepolárních vitamínů., This thesis deals with the characterization and preparation of catanionic vesicular systems and their interaction with water-insoluble vitamins. Catanionic vesicles systems was prepared from two differently charged sufractants CTAB and SDS in formation ion pair amphiphile. Stability of vesicles was secured by adding cholesterol with positively charged surfactant DODAC. Were selected vitamin A and vitamin E for solubilization into these vesicles. The next part of this work was focused on determining the efficiency of incorporation these vitamins into the HTMA-DS vesicular system. The characterization of these systems was improved by measurement on a UV-VIS spectrometer, DLS and by HPLC with UV-VIS detector. During measurement by UV-VIS and HPLC the efficiency of solubilization of vitamin A and vitamin E into vesicles was determinated. In both cases higher efficiency was determinated for vesicles with incorporated vitamin A. Higher efficiency for both vitamins was determinated by HPLC. The reason is probably the higher sensitivity of the metod, work in labs with dark glass and preparing individuals samples into vials, which were inserted into the device for individual dosing by injector. The work serves primary evaluation results in view of the vesicular system for use in pharmaceutical application like carrier non-polar vitamins.

Tato diplomová práce se zabývá studiem inkorporace nízko a vysokomolekulárních látek do liposomálních systémů. Cílem práce bylo stanovit enkapsulační účinnost (EE) vybraných látek a vliv jednotlivých komponent liposomálního systému na EE. Liposomy byly připraveny z dipalmitoylfosfatidylcholinu, stabilizovány byly přídavkem cholesterolu a přídavkem kyseliny fosfatidové získaly záporný náboj. Stealth vlastnosti získaly navázáním polyethylenglykolu a přídavkem trimethylchitosanu byl umožněn vstup liposomů do krevního řečiště paracelulární cestou. K inkorporaci do liposomů byl použit vitamín C a enzym bromelain. Ke zjištění enkapsulační účinnosti liposomů připravených kombinací jednotlivých složek byla použita metoda UV-VIS spektrofotometrie. Bylo zjištěno, že vitamín C a enzym lze inkorporovat do liposomů, kdy enzym vykazuje vyšší EE. Dále bylo zjištěno, že největší vliv na EE má kyselina fosfatidová a trimethylchitosan, který zvyšuje EE vitamínu C a naopak snižuje EE enzymu., This master´s thesis deals with the study of the incorporation of low and high molecular weight substances into liposomal systems. The aim of the work was to determine the encapsulation efficiency (EE) of the active substance and the influence of individual components of the liposomal system on EE. Liposomes were prepared from dipalmitoylphosphatidylcholine. They were stabilized by cholesteroland and phosphatidic acid was added to give a negative charge. Stealth properties gain the binding of polyethylene glycol and other trimethyl chitosan we enabled the entry of liposomes into the bloodstream by the paracellular pathway. Vitamin C and the enzyme bromelain were used for incorporation into liposomes. UV-VIS spectrophotometry was used to determine the encapsulation efficiency of liposomes prepared by combining the individual components. It has been suggested that vitamin C and the enzyme can be incorporated into liposomes, but an enzyme with a higher EE. Furthermore, phosphatidic acid and trimethyl chitosan have been found to affect EE, which increases the EE of vitamin C and decreases the EE of the enzyme.

Tato diplomová práce se zabývá studiem inkorporace nízko a vysokomolekulárních látek do liposomálních systémů. Cílem práce bylo stanovit enkapsulační účinnost (EE) vybraných látek a vliv jednotlivých komponent liposomálního systému na EE. Liposomy byly připraveny z dipalmitoylfosfatidylcholinu, stabilizovány byly přídavkem cholesterolu a přídavkem kyseliny fosfatidové získaly záporný náboj. Stealth vlastnosti získaly navázáním polyethylenglykolu a přídavkem trimethylchitosanu byl umožněn vstup liposomů do krevního řečiště paracelulární cestou. K inkorporaci do liposomů byl použit vitamín C a enzym bromelain. Ke zjištění enkapsulační účinnosti liposomů připravených kombinací jednotlivých složek byla použita metoda UV-VIS spektrofotometrie. Bylo zjištěno, že vitamín C a enzym lze inkorporovat do liposomů, kdy enzym vykazuje vyšší EE. Dále bylo zjištěno, že největší vliv na EE má kyselina fosfatidová a trimethylchitosan, který zvyšuje EE vitamínu C a naopak snižuje EE enzymu., This master´s thesis deals with the study of the incorporation of low and high molecular weight substances into liposomal systems. The aim of the work was to determine the encapsulation efficiency (EE) of the active substance and the influence of individual components of the liposomal system on EE. Liposomes were prepared from dipalmitoylphosphatidylcholine. They were stabilized by cholesteroland and phosphatidic acid was added to give a negative charge. Stealth properties gain the binding of polyethylene glycol and other trimethyl chitosan we enabled the entry of liposomes into the bloodstream by the paracellular pathway. Vitamin C and the enzyme bromelain were used for incorporation into liposomes. UV-VIS spectrophotometry was used to determine the encapsulation efficiency of liposomes prepared by combining the individual components. It has been suggested that vitamin C and the enzyme can be incorporated into liposomes, but an enzyme with a higher EE. Furthermore, phosphatidic acid and trimethyl chitosan have been found to affect EE, which increases the EE of vitamin C and decreases the EE of the enzyme.

Tato bakalářská práce se zabývá studiem enkapsulační účinnosti hydrofilní látky a jejím uvolňováním z vodného středu v závislosti na odlišném složení komponent jednotlivých lipozomálních systémů. Jako modelové léčivo byla vybrána hydrofilní fluorescenční sonda zvaná pyranin. Cílem bylo připravit lipozomy, které by byly z hlediska jejich vlastností vhodné pro inhalační podávání a které by zajistily pasivní cílení s prodlouženou dobou uvolňování bez vyvolání vedlejších účinků na organismus. Podařilo se nám vytvořit standardní operační postup pro inkorporaci hydrofilních látek. Byly připraveny lipozomální systémy skládající se z přídavků různých komponent, jako je cholesterol, kyselina fosfatidová, polyethylenglykol navázaný na fosfatidylethanolamin a trimethylchitosan. Dále se nám podařilo charakterizovat jednotlivé lipozomální systémy z hlediska velikosti, stability a enkapsulační účinnosti, což jsou důležité fyzikálně-chemické vlastnosti pro další aplikační potenciál., This bachelor thesis deals with the study of the encapsulation efficiency of hydrophilic drugs and their releasing from the aqueous core depending on the different composition of the components of individual liposomal systems. The hydrophilic fluorescent probe called pyranine was chosen as a model drug. The aim was to prepare liposomes which would be suitable for inhalation administration in terms of their properties. These liposomes would provide passive targeting with prolonged release time without causing negative side effects on the organism. We have succeeded in developing a standard operating procedure for the incorporation of hydrophilic drugs. Liposomal systems have been prepared consisting of the addition of various components as cholesterol, phosphatidic acid, pegylated phosphatidylethanolamine and trimethylchitosan. Furthermore, we were able to characterize the individual liposomal systems in terms of size, stability and encapsulation efficiency which are important physicochemical properties for further application potential.

Tato diplomová práce se zabývá studiem enkapsulační účinnosti antibiotika doxycyklinu v lipozomálních systémech s odlišným složením komponent. Pojednává i o kinetice uvolňování enkapsulovaného léčiva z těchto nosičových systémů. Lipozomální systémy pro léčbu lokálních plicních onemocnění byly vybrány na základě vhodných fyzikálně chemických vlastností. Jako mikroorganismus, který modeluje lokální plicní onemocnění, plicní pneumonii, byla vybrána bakterie Staphylococcus aureus. Doxycyklin byl zvolen jako antibiotikum ideální pro léčbu stafylokokové infekce. Cílem bylo optimalizovat složení lipozomů tak, aby měly lipozomální systémy aplikační potenciál pro inhalační podávání léčiv. Byly připraveny dva vhodné lipozomální systémy skládající se z přídavků cholesterolu a kyseliny fosfatidové. Podařilo se nám určit koncentraci léčiva pro enkapsulaci, která měla dostatečnou antimikrobiální účinnost pro léčbu lokálního plicního onemocnění. Ke stanovení vedlejších účinků zvolených lipozomálních systémů byly využity cytotoxické testy. Dále byly jednotlivé lipozomální systémy charakterizované z hlediska velikosti, zeta potenciálu a kinetické stability, což jsou další důležité vlastnosti ovlivňující jejich budoucí aplikační potenciál., This diploma thesis deals with the study of the encapsulation efficiency of the antibiotic doxycycline encapsulated in the individual liposomal systems depending on different composition of the components. We also discussed the kinetics of the encapsulated drug releasing from the carrier systems. The liposomal systems for the treatment of local lung diseases were selected due to their suitable physicochemical properties. The bacterium called Staphylococcus aureus was chosen as a model of the local lung disease, pulmonary pneumonia. Doxycycline was chosen as the antibiotic ideal for the treatment of staphylococcal infection. The aim of the diploma thesis was to optimize the composition of liposomes which would have application potential for the inhalation administration of drugs. Two suitable liposomal systems have been prepared consisting of the addition of various components as cholesterol and phosphatidic acid. We have succeeded in determination of the drug concentration for the encapsulation which had sufficient antimicrobial efficacy to treat the local lung disease. The cytotoxic tests were used to determine the side effects of selected liposomal systems. Furthermore, the individual liposomal systems were characterized in terms of size, zeta potential and kinetic stability which are other important properties effecting their future application potential.

Tato diplomová práce se zabývá charakterizací a přípravou kataniontových vezikulárních systémů a jejich následnou interakcí s ve vodě nerozpustnými vitamíny. Kataniontové vezikulární systémy byly připraveny z dvou různě nabitých povrchově aktivních látek CTAB a SDS za vzniku iontového amfifilního páru. Stabilita vezikul byla zajištěna přidáním cholesterolu spolu s kladně nabitou povrchově aktivní látkou DODAC. Pro následnou solubilizaci do těchto vezikul byl vybrán vitamín A a vitamín E. Další část práce byla zaměřena na stanovení efektivity inkorporace těchto vitamínů do vezikulárních systémů HTMA-DS. Charakterizace těchto systémů byla provedena pomocí měření na UV-VIS spektrometru, DLS a pomocí HPLC s UV-VIS detektorem. Během měření na UV-VIS a HPLC byla stanovena účinnost solubilizace vitamínu A a vitamínu E do vezikul. V obou případech byla stanovena vyšší účinnost u vezikul s inkorporovaným vitamínem A. Vyšší účinnost u obou vitamínů byla stanovena pomocí metody HPLC. Důvodem je pravděpodobně vyšší citlivost metody, práce s tmavým sklem a příprava jednotlivých vzorků do vialek, které byly následně vloženy do přístroje pro jednotlivé dávkování pomocí injektoru. Práce slouží především ke zhodnocení výsledků z hlediska použitelnosti daného vezikulárního systému za účelem uplatnění ve farmaceutických aplikacích jako nosiče nepolárních vitamínů., This thesis deals with the characterization and preparation of catanionic vesicular systems and their interaction with water-insoluble vitamins. Catanionic vesicles systems was prepared from two differently charged sufractants CTAB and SDS in formation ion pair amphiphile. Stability of vesicles was secured by adding cholesterol with positively charged surfactant DODAC. Were selected vitamin A and vitamin E for solubilization into these vesicles. The next part of this work was focused on determining the efficiency of incorporation these vitamins into the HTMA-DS vesicular system. The characterization of these systems was improved by measurement on a UV-VIS spectrometer, DLS and by HPLC with UV-VIS detector. During measurement by UV-VIS and HPLC the efficiency of solubilization of vitamin A and vitamin E into vesicles was determinated. In both cases higher efficiency was determinated for vesicles with incorporated vitamin A. Higher efficiency for both vitamins was determinated by HPLC. The reason is probably the higher sensitivity of the metod, work in labs with dark glass and preparing individuals samples into vials, which were inserted into the device for individual dosing by injector. The work serves primary evaluation results in view of the vesicular system for use in pharmaceutical application like carrier non-polar vitamins.