Search

The objective of this work is to investigate the nanoencapsulation of valuable bioactive compounds with the innovative electrohydrodynamic technology. More specifically, electrospraying, was applied for the encapsulation of three different active agents with lipolytic, anti-aging and antioxidant activity: Deoxycholic acid (DCA), olive leaves’ enzymatically modified extract and a hybrid of Deoxycholic acid-Hydroxytyrosol (DCA-HXT) in zein (ZN) biodegradable polymer. The resulting powders were evaluated regarding the system's: compositional and chemical characteristics, thermal stability and humidity effect, morphology, shape and size, encapsulation efficiency and release kinetics from the wall material. Encapsulation led to stable nanosystems, regarding the moisture and temperature effect, with high glass Transition Temperatures (Tg between 130-139 °C), and a mean particle size of 400-600 nm. Finally, high encapsulation efficiencies (DCA= 84.01%, DCA-HXT = 79.34% and modified extract =80.75%) and long-term release profiles (DCA=192 h, DCA-HXT=228 h and mod. extract=100 h) were measured for all three systems. Based on these results, we conclude that electrospraying process is an effective methodology for the development of bioactive agents’ nanosystems with excellent physicochemical properties and increased bioavailability; a crucial factor for the formation of high added-value products such as cosmetics.

Anthocyanins are important phytochemical compounds in nature that are of interest not only for their health benefits such as antioxidant, anti‐inflammatory, and anti‐carcinogenic properties, but also for their role in imparting attractive and characteristic color to food products. In this study, anthocyanins from hibiscus (Hibiscus sabdariffa L.) calyces were microencapsulated by spray‐drying technique using maltodextrin as the carrier. The experiment was carried out in the full factorial design with two factors, namely inlet temperature (150, 160, and 170°C) and anthocyanin to maltodextrin mass ratio (1:50, 1:60, 1:70, 1:80, 1:90, and 1:100) with the aim of investigating the effect of spray drying conditions on phenolic content, anthocyanin, antioxidant activity, and color of spray‐dried hibiscus powder. The results showed that increasing the carrier ratio significantly reduced the antioxidant content and their activities in the powder. However, the high level of carriers exhibited a protective effect in encapsulating anthocyanin compounds into the maltodextrin matrix, which was demonstrated by high encapsulation efficiency (>85%) observed in the samples prepared at a ratio of 1:100. It should be highlighted that although high temperature (170°C) reduced total anthocyanin concentration, it actually enhanced total phenolic content. In addition, the moisture content of the powder declined with increasing carrier ratio and inlet temperature, and it was found to be in the range of 5.57%–10.19% in the powder. With solubility greater than 93.71%, the total phenolic and total anthocyanin content of spray‐dried hibiscus powder were 31.5–41.9 (mg gallic acid equivalent/g of dry powder) and 6.08–10.47 (mg cyanidin‐3‐glucoside/g of dry powder), respectively.

An in situ streptavidin‐encapsulated hydrogel based on dendritic polyglycerol (dPG) which is functionalized with either an acrylate, allyl or acrylamide group and dithiolated polyethylene glycol (PEG) is constructed via a thiol‐click chemistry approach and is investigated for biosensing applications. The hydrogel platform is screened for the encapsulation and release efficiencies of the model protein streptavidin under varying physicochemical conditions, for example, crosslinking chemistry reactions, the molar ratio between the two gel components, macromonomer concentrations or pH‐values. By that, tailor‐made hydrogels can be developed, which are able to encapsulate or release the model protein for several days based on its modality. Furthermore, the accessible binding site of encapsulated streptavidin or in other words, the biotin‐binding performance is quantified, and the stability of the various hydrogel types is studied by rheology measurements, 1H NMR, gel permeation chromatography (GPC), and mass loss experiments.

Rapid release and diminished stability are two of the limitations associated with the growth factors that are essentially used in dental applications. These growth factors are employed to enhance the quality and quantity of tissue or bone matter during regeneration. Therefore, drug delivery devices and systems have been developed to address these limitations. In this study, bovine serum albumin (BSA), as a representative growth factor, was successfully sustained by encapsulation with the medium-absorbable copolymer, poly(L-lactide-co-glycolide) (PLG) 70:30% mol, via the multiple emulsion method. Different PLG, PVA, and BSA concentrations were used to investigate their effects on the BSA encapsulation efficiency. The suitable ratios leading to a better characterization of microparticles and a higher encapsulation efficiency in producing encapsulated PLG microparticles were 8% (w/v) of PLG, 0.25% (w/v) of PVA, and 8% (w/v) of BSA. Furthermore, an in vitro release study revealed a bursting release of BSA from the encapsulated PLG microsphere in the early phase of development. Subsequently, a gradual release was observed over a period of eight weeks. Furthermore, to encapsulate LL-37, different proteins were used in conjunction with PLG under identical conditions with regard to the loading efficiency and morphology, thereby indicating high variations and poor reproducibility. In conclusion, the encapsulated PLG microparticles could effectively protect the protein during encapsulation and could facilitate sustainable protein release over a period of 60 days. Importantly, an optimal method must be employed in order to achieve a high degree of encapsulation efficiency for all of the protein or growth factors. Accordingly, the outcomes of this study will be useful in the manufacture of drug delivery devices that require medium-sustained release growth factors, particularly in dental treatments.

Proteins are bioactive compounds with high potential to be applied in the biopharmaceutical industry, food science and as biocatalysts. However, protein stability is very difficult to maintain outside of the native environment, which hinders their applications. Fluorinated ionic liquids (FILs) are a promising family of surface-active ionic liquids (SAILs) that have an amphiphilic behavior and the ability to self-aggregate in aqueous solutions by the formation of colloidal systems. In this work, the protein lysozyme was selected to infer on the influence of FILs in its stability and activity. Then, the cytotoxicity of FILs was determined to evaluate their biocompatibility, concluding that the selected compounds have neglected cytotoxicity. Therefore, UV–visible spectroscopy was used to infer the FIL-lysozyme interactions, concluding that the predominant interaction is the encapsulation of the lysozyme by FILs. The encapsulation efficiency was also tested, which highly depends on the concentration and anion of FIL. Finally, the bioactivity and thermal stability of lysozyme were evaluated, and the encapsulated lysozyme keeps its activity and thermal stability, concluding that FILs can be a potential stabilizer to be used in protein-based delivery systems. publishersversion published

Lupeol liposomes, modified with Gal-PEG-DSPE, were developed following a thin-film dispersion method. Then, the morphology, physicochemical properties, and in vitro release properties of those liposomes were investigated. The scanning electron microscopic images showed that most of the liposomes were spherical particles; they were similar in size and uniformly dispersed. Both lupeol liposomes and Gal-lupeol liposomes exhibited an average particle size of about 100 nm. The encapsulation efficiency was greater than 85%. The encapsulation efficiency of lupeol liposome and Gal-lupeol liposome, stored with 15% sucrose as glycoprotein for 6 months, was higher than 80%; although the particle size increased, they remained within 200 nm. The cell-uptake study demonstrated that the Gal-lupeol-liposome uptake efficiency was the highest in HepG2 cells. The HepG2 cells treated with the Gal-lupeol liposomes had higher apoptotic efficiency than the lupeol liposome and free lupeol. After HepG2 cells were treated with Gal-lupeol liposome, the expressions of AKT/mTOR-related proteins (p-AKT308 and p-AKT473) were also significantly reduced than the lupeol-liposome and free lupeol group. The in vivo targeting studies showed that Gal-NR-L exhibited liver-targeting effects on FVB mice. The pharmacodynamic study was performed by transfecting AKT and c-MET via the high-pressure tail vein of FVB mice. After Gal-lupeol-L administration, the liver index and liver weight of mice were less than those non-targeted group. The histopathological study showed that the lobular structure in the mice liver was clearer, the vacuoles were more obvious, and the cytoplasm was more abundant after Gal-lupeol-L administration. Also, the qRT-PCR study showed that AFP, GPC3, and EpCAM mRNA expression levels were significantly lower than those non-targeted lupeol-liposomes.

Maltodextrin, modified starch, inulin, alginate, gum arabic, and combinations thereof were used as carrier agents for spray drying of carotenoid-rich goldenberry (Physalis peruviana L.) juice and compared to cellobiose as an alternative carrier. Powders were analyzed with respect to particle size and morphology, yield, moisture content, cold water solubility, suspension stability, hygroscopicity, carotenoid encapsulation efficiency, and carotenoid retention during storage. A high initial carotenoid concentration after spray drying, a high encapsulation efficiency of 77.2%, and a slow carotenoid degradation kinetics favored the high carotenoid content of the cellobiose powder at the end of the storage. Cellobiose might protect the carotenoids from degradation processes by light exposure, high temperature, and oxygen due to a tighter particle crust and larger particle sizes. Therefore, cellobiose may be considered a potential carrier agent for the encapsulation of carotenoid-rich fruit juices., Graphical abstract Image 1, Highlights • Goldenberry juice was spray dried with different carrier agents. • Cellobiose was used as carrier agent in the present study for the first time. • The cellobiose powder provided the best retention of carotenoids. • Spray drying promoted isomerization reactions of all-trans-β-carotene. • Cellobiose proved to be effective for spray drying of carotenoid-rich juices.

In this work, a series of nanoencapsulated phase change materials (NanoPCMs) with paraffin wax (PW) as core and melamine-formaldehyde (MF) as shell were synthesized by the in-situ polymerization method. The morphology, chemical structure and thermal properties of prepared NanoPCMs were characterized by scanning electron microscope, Fourier transform infrared, differential scanning calorimetry and thermogravimertic analyzer. The results show that the PW is successfully encapsulated in the MF without chemical interaction, and the NanoPCMs present regular spherical shape with the average diameter of 260–450 nm. The encapsulation efficiency of the NanoPCMs increases with the augment of the supplied amount of core material. The maximum encapsulation efficiency of the NanoPCMs can reach up to approximately 75%. The NanoPCMs can maintain excellent thermal reliability and stability after 2000 thermal cycling. The prepared NanoPCMs can be well applied in the latent heat thermal energy storage and thermal management systems due to their remarkable encapsulation efficiency and thermal properties enable them to.

Introduction . Drug encapsulation efficiency (EE) is the important parameter of the nanoparticle-based drug formulations. Generally, the methods for evaluation of the EE are based on separation of the free and NP-bound fractions of the drug; however, applicability of these methods for a particulate formulation needs careful consideration. Aim. The purpose of the study was to optimize the procedure for evaluation of the EE for a nanoparticle-based drug formulation taking doxorubicin loaded in the PLGA nanoparticles (PLGA-Dox NP) as a model formulation. Materials and methods. The PLGA-Dox NP were prepared by a “double emulsion” method at pH of the external aqueous phase of 7.4 or 6.4. The NP size and size distribution (PDI) were determined by photon correlation spectroscopy (PCS) and transmission electron microscopy (TEM). For the EE evaluation of doxorubicin, the NP were separated by centrifugation (CF), ultrafiltration (UF), or gel filtration. The efficiency of NP separation by the CF method was evaluated by the PLGA content in the supernatant by capillary electrophoresis (CZE). Results and discussion. The average hydrodynamic diameter of the PLGA-Dox/7.4 and PLGA-Dox/6.4 NP (FCS) was 103 ± 10 nm and 141 ± 8 nm, respectively. According to the TEM data, the main fraction of the NP averaged 50 ± 16 nm. The EE of doxorubicin, determined after the NP separation by centrifugation at 48254.g, was 78.9 ± 1.8 % for the PLGA-Dox/6.4 and 91.5 ± 0.9 % for the PLGA-Dox/7.4 NP with the residual PLGA content in the supernatant of ~5 %. At lower acceleration the NP separation was incomplete leading to underestimation of the EE. Also, the ultrafiltration method using the filters with the NMWL of 50 and 100 kDa enabled the reliable NP separation with the minimal doxorubicin adsorption on the filter (

The most widely-used wall materials for spray-dried microencapsulation have limitations in cost-effectiveness, health benefits and sustainability. Wood hemicelluloses, by-products of the forestry industry, including gal-actoglucomannans and glucuronoxylans have the potential to be utilized as innovative wall materials. This study investigated the applicability of galactoglucomannan and glucuronoxylan and their mixtures with carboxy-methylcellulose as wall materials for microencapsulation of bilberry juice, in comparison to gum arabic. The results indicated that galactoglucomannan and glucuronoxylan have a relatively high anthocyanin encapsulation efficiency (71-73%), which was similar to that of gum arabic (76%). The addition of carboxymethylcellulose reduced the encapsulation efficiency of wood hemicelluloses to 46-54%. Microencapsulated powders prepared with wood hemicelluloses were considerably higher in total phenolic content and antioxidant activities than those prepared with gum arabic, and mixtures of wood hemicelluloses with carboxymethylcellulose. The results indicate that wood hemicelluloses are efficient wall materials for spray-dried microencapsulation of bioactive compounds.

For improving solubility and bioaccessibility of phytosterols (PS), phytosterol nanoparticles (PNPs) were prepared by emulsification–evaporation combined high-pressure homogenization method. The organic phase was formed with the dissolved PS and soybean lecithin (SL) in anhydrous ethanol, then mixed with soy protein isolate (SPI) solution, and homogenized into nanoparticles, followed by the evaporation of ethanol. The optimum fabrication conditions were determined as PS (1%, w/v): SL of 1:4, SPI content of 0.75% (w/v), and ethanol volume of 16 ml. PNPs were characterized to have average particle size 93.35 nm, polydispersity index (PDI) 0.179, zeta potential −29.3 mV, and encapsulation efficiency (EE) 97.3%. The impact of temperature, pH, and ionic strength on the stability of fabricated PNPs was determined. After 3-h in vitro digestion, the bioaccessibility of PS in nanoparticles reached 70.8%, significantly higher than the 18.2% of raw PS. Upon freeze-drying, the particle size of PNPs increased to 199.1 nm, resulting in a bimodal distribution. The solubility of PS in water could reach up to 2.122 mg/ml, ~155 times higher than that of raw PS. Therefore, this study contributes to the development of functional PS-food ingredients.

Edible nanoparticles containing antibacterial agents are one of the effective strategies to control foodborne diseases. Herein, novel ternary nanoparticles (TNP) were prepared from rosemary essential oil (REO), nisin and Lycium barbarum polysaccharides (LBP) through hydrophobic and electrostatic interaction. The average particle size of TNP was 211.5 nm, and its encapsulation efficiency reached 86.6%. After the addition of LBP, the physical stability, thermal stability and storage stability of TNP were significantly improved. In vitro, compared with the control group, the population of S. aureus and E. coli O157:H7 in the TNP-treated group was reduced by 2.386 log CFU/mL and 1.966 log CFU/mL, respectively, on the fifth day. The free radical scavenging rate of TNP was 63.15%. The application of TNP on beef presented favorable preservation effects without affecting its color and texture. Therefore, the synthesis strategy of TNP has important reference significance for the research and development of new food antibacterial agents.

The encapsulation efficiency (EE%) and structural changes within the Anthraquinones-encapsulated casein micelles (CM) powders were evaluated in this study. For this purpose, the anthraquinone powder extracted from Aloevera, its freeze-dried powder (FDP) and whole leaf Aloe vera gel (WLAG) has been encapsulated in CM through ultrasonication prior to spray dying to produce nanocapsules: CM encapsulated anthraquinone powder (CMAQP), CM encapsulated freeze-dried powder (CMFDP) and CM encapsulated Whole leaf aloe vera gel (CMWLAG). Based on the pH of the solution before drying, CMAQP had the highest EE% following spray drying. However, due to air-interface-related dehydration stresses, SD resulted in a slight decrease in the EE% of anthraquinones (aloin, aloe-emodin, and rhein) in CMAQP. Meanwhile, a significant increase in EE% of CMFDP was observed compared to the aqueous state. According to SEM findings, the particle size of CMAQP was 2.39 µm and ξ-potential of ~−17mV. The CMFDP had a rough fractal surface with large particle sizes and potential of 3.49 µm and ~−11mV respectively. CM deformed, having the least EE% and lowest ξ-potential (−4.5 mV). Spray drying enhances melanoidin formation in CMWLAG, as evidenced by the highest chroma values. The results suggested that EE%, stability, and degree of Maillard reaction are closely linked to the type of anthraquinone encapsulated, the pH of the solution, and the nanostructure of casein micelles during spray drying.

Anthocyanins are important phytochemical compounds in nature that are of interest not only for their health benefits such as antioxidant, anti‐inflammatory, and anti‐carcinogenic properties, but also for their role in imparting attractive and characteristic color to food products. In this study, anthocyanins from hibiscus (Hibiscus sabdariffa L.) calyces were microencapsulated by spray‐drying technique using maltodextrin as the carrier. The experiment was carried out in the full factorial design with two factors, namely inlet temperature (150, 160, and 170°C) and anthocyanin to maltodextrin mass ratio (1:50, 1:60, 1:70, 1:80, 1:90, and 1:100) with the aim of investigating the effect of spray drying conditions on phenolic content, anthocyanin, antioxidant activity, and color of spray‐dried hibiscus powder. The results showed that increasing the carrier ratio significantly reduced the antioxidant content and their activities in the powder. However, the high level of carriers exhibited a protective effect in encapsulating anthocyanin compounds into the maltodextrin matrix, which was demonstrated by high encapsulation efficiency (>85%) observed in the samples prepared at a ratio of 1:100. It should be highlighted that although high temperature (170°C) reduced total anthocyanin concentration, it actually enhanced total phenolic content. In addition, the moisture content of the powder declined with increasing carrier ratio and inlet temperature, and it was found to be in the range of 5.57%–10.19% in the powder. With solubility greater than 93.71%, the total phenolic and total anthocyanin content of spray‐dried hibiscus powder were 31.5–41.9 (mg gallic acid equivalent/g of dry powder) and 6.08–10.47 (mg cyanidin‐3‐glucoside/g of dry powder), respectively., Increasing the carrier ratio reduced antioxidant contents and activities. High inlet temperature effectively retained phenolic compounds. High encapsulation efficiency of anthocyanin (above 85%) was obtained at an ACN:MD ratio of 1:100 (w/w). Increasing carrier ratio and inlet temperature resulted in decrease in moisture content, and the solubility of all samples exceeded 93.71%.

Methotrexate (MTX) anticancer drug was successfully loaded and released in a controlled manner from polymer micelles made of a diblock copolymer of poly(monomethoxy ethylene glycol)-b-poly(ε-caprolactone) (mPEG-PCL). The empty and MTX-loaded micelles (MTX/mPEG-PCL) were characterized by electron microscopy. The drug release dependence upon pH 5.4, 6.5, and 7.4 for 30 days was proven and characterized by UV-Vis spectroscopy. The cytotoxic effect of MTX/mPEG-PCL micelles on MCF-7 breast cancer cells was evaluated through an MTT assay. The morphological analysis indicated the successful formation of micelles of 76 and 131 nm for empty and MTX-loaded micelles, respectively. An encapsulation efficiency of 70.2% and a loading capacity of 8.8% were obtained. The in vitro release of MTX showed a gradual and sustained profile over 22 days, with a clear trend to much higher release at acidic pH (80 and 90% for pH 6.7 and 5.5, respectively). The MTX/mPEG-PCL micelles showed an IC50 of MCF-7 cells at 30 µg mL−1. The results suggested that MTX/mPEG-PCL could be a promising drug delivery system for cancer treatment.

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.

In this study, it was aimed to prepare and characterize double (W1/O/W2) emulsions for encapsulation of ferric chloride within the internal aqueous phase (W1). The primary (W1/O) emulsion to be used in double emulsion was examined for oxidative stability and whey protein isolate was found effective in improving oxidation stability. The double emulsions were prepared with different primary emulsion:external water phase (W1/O:W2) ratios as 40:60, 30:70 and 20:80; the emulsions were characterized in terms of droplet size, encapsulation efficiency, rheology, creaming stability and in vitro iron bioaccessibility. The emulsion with 40:60 ratio had the highest viscosity and encapsulation efficiency whereas it had the lowest creaming index and droplet size. It was also obtained that iron bioaccessibility increased as the ratio of W2 phase increased and the double emulsion with 20:80 ratio showed the highest bioaccessibility (52.97 ± 0.89%). This study may enable the use of double emulsion encapsulation in the enrichment of food products with iron. © 2019 Elsevier Ltd, 114O209, The authors gratefully acknowledge the financial support provided by TUBITAK (Project no: 114O209 ).

Herein we investigated the utilization of various encapsulation materials of blue pigments phycocyanin from Arthrospira platensis extract by spray drying to ensure the stability in foods. Various combinations and ratios of wall materials (maltodextrin, gum arabic, whey protein isolate, and sodium caseinate) were tried to examine the emulsion characterization, physical properties, and efficiency of the microcapsules. The moisture content and water activity of the microcapsules having different wall materials were quite similar to each other. However, wall material type and ratio significantly affected the solubility, color values, and microencapsulation efficiency. While the highest microencapsulation efficiency (91.19% +/- 0.88%) was achieved with a combination of gum arabic and whey protein isolate as wall material, the highest blueness index was observed in phycocyanin powder encapsulated with maltodextrin and whey protein isolate. Novelty impact statement Microencapsulation by spray drying method was preferred for protecting phycocyanin from external factors that improve its stability. The effect of typical wall materials based on carbohydrate (maltodextrin, gum arabic) and protein based (whey protein isolate, sodium caseinate) on the feed emulsion and the properties of the final powder product was investigated in detail. In the development of microcapsules, the highest microencapsulation efficiency was obtained in gum arabic and cheese protein isolate, but combinations of maltodextrin and whey protein isolate wall material, attractive blue color, and acceptable microencapsulation efficiency were achieved., COST Action [ES1408]; Scientific and Technological Research Council of Turkey [TUBITAK--115O578], This study was a part of COST Action ES1408. The authors would like to thank The Scientific and Technological Research Council of Turkey (TUBITAK--115O578) for financial support.

Purpose Opioids have been the main factor for drug overdose deaths in the United States. Current naloxone delivery systems are effective in mitigating the opioid effects only for hours. Naloxone-loaded poly(lactide-co-glycolide) (PLGA) microparticles were prepared as quick- and long-acting naloxone delivery systems to extend the naloxone effect as an opioid antidote. Methods The naloxone-PLGA microparticles were made using an emulsification solvent extraction approach with different formulation and processing parameters. Two PLGA polymers with the lactide:glycolide (L:G) ratios of 50:50 and 75:25 were used, and the drug loading was varied from 21% to 51%. Two different microparticles of different sizes with the average diameters of 23 μm and 50 μm were produced using two homogenization-sieving conditions. All the microparticles were critically characterized, and three of them were evaluated with β-arrestin recruitment assays. Results The naloxone encapsulation efficiency (EE) was in the range of 70–85%. The EE was enhanced when the theoretical naloxone loading was increased from 30% to 60%, the L:G ratio was changed from 50:50 to 75:25, and the average size of the particles was reduced from 50 μm to 23 μm. The in vitro naloxone release duration ranged from 4 to 35 days. Reducing the average size of the microparticles from 50 μm to 23 μm helped eliminate the lag phase and obtain the steady-state drug release profile. The cellular pharmacodynamics of three selected formulations were evaluated by applying DAMGO, a synthetic opioid peptide agonist to a μ-opioid receptor, to recruit β-arrestin 2. Conclusions Naloxone released from the three selected formulations could inhibit DAMGO-induced β-arrestin 2 recruitment. This indicates that the proposed naloxone delivery system is adequate for opioid reversal during the naloxone release duration.

Orientador: Miriam Dupas Hubinger Dissertação (mestrado) - Universidade Estadual de Campinas, Faculdade de Engenharia de Alimentos Resumo: O presente trabalho teve como objetivo o estudo da microencapsulação do óleo de café através de secagem por atomização. Inicialmente, foram avaliadas as variáveis de concentração de sólidos, concentração de óleo em relação aos sólidos e temperatura na secagem por spray dryer, através de um delineamento experimental composto central rotacional completo (23), usando goma arábica como material de parede, sobre as seguintes respostas: umidade, densidade aparente, higroscopicidade, óleo superficial, óleo total, retenção de óleo e eficiência de encapsulação. Nas condições otimizadas do planejamento (30% de sólidos, 15% de óleo em relação aos sólidos e 170º C) foi avaliado o efeito da homogeneização da emulsão a alta pressão (200, 600 e 1000 bar) nas características do pó, comparando-o com o pó obtido a partir de emulsão homogeneizada com o uso de um homogeneizador do tipo rotor-estator. A aplicação de alta pressão reduziu o tamanho das partículas da emulsão, aumentou a eficiência de encapsulação e reduziu o tamanho das partículas do pó, contudo reduziu a retenção de óleo. Ainda, nas mesmas condições selecionadas no planejamento, foram avaliados diferentes materiais de paredes combinados (proteína de soro de leite isolada e maltodextrina; goma arábica e maltodextrina) em diferentes razões (3:1, 1:1 e 1:3) ou puros (goma arábica e proteína de soro de leite). O emprego de materiais de parede diferentes resultou em alterações na viscosidade, no tamanho das gotas das emulsões, na higroscopicidade, densidade e molhabilidade. A mistura de proteína e maltodextrina resultou em alta eficiência de encapsulação e mostrouse como uma possível substituta para a goma arábica. Em seguida, avaliou-se a estabilidade das microcápsulas produzidas com diferentes materiais de parede (goma arábica, maltodextrina e proteína de soro de leite - nas razões 3:1, 1:1, 3:1- e proteína de soro de leite), através da construção de isotermas de sorção e determinação da temperatura de transição vítrea. As microcápsulas produzidas com proteína apresentaram baixa higroscopicidade e alta estabilidade mesmo em ambientes com alta umidade relativa. Foi ainda avaliada a estabilidade oxidativa do óleo de café puro e microencapsulado com diferentes materiais de parede às temperaturas de 25 e 60º C. Tanto o óleo de café puro quanto o microencapsulado apresentaram alta estabilidade oxidativa a 25º C. Já as amostras armazenadas a 60º C apresentaram maiores valores de índice de peróxidos, contudo observou-se uma melhora, ainda que pequena, na estabilidade oxidativa do óleo de café microencapsulado em relação à do óleo puro Abstract: The objective of this work was studying coffee oil microencapsulation by means of spray drying. Initially, the solid concentration, oil concentration in relation to solids and drying temperature were evaluated by using a complete central rotational experimental design (23), using arabic gum as wall material, on the following responses: moisture content, bulk density, hygroscopicity, superficial oil, total oil, oil retention and encapsulation efficiency. Using the planning optimized conditions (30% of solids, 15% of oil in relation to solids, and 170º C) the effect of high-pressure homogenization (200, 600 and 1000 bar) on the powder characteristics was evaluated in comparison with the powder obtained from a homogenized emulsion with the use of a rotor-stator homogenizer. The use of high-pressure reduced the size of emulsion particles, increased encapsulation efficiency and reduced powder particle size; however, it also reduced oil retention. Applying the same conditions selected in the planning, different combined wall materials were evaluated (isolated whey protein and maltodextrin; arabic gum and maltodextrin) in different ratios (3:1, 1:1 and 1:3) or pure (arabic gum and isolated whey protein). The use of different wall materials resulted in changes on viscosity, emulsion particle size and powder's properties, such as hygroscopicity, density and wettability. The combination of protein and maltodextrin resulted in higher encapsulation efficiency and proved itself as a possible substitute for arabic gum. Further, the stability of microcapsules made of different wall materials (arabic gum, maltodextrin and whey protein - in rates 3:1, 1:1 and 1:3- and sole whey protein) was evaluated, by the construction of sorption isotherms and glass transition temperature determination. The microcapsules made of protein presented low hygroscopicity and stability, even in high relative humidity environments. Finally, the oxidative stability of pure and microencapsulated coffee oil with different wall materials was analyzed at 25 and 60º C. Both pure coffee oil and the microencapsulated one presented high oxidative stability at 25º C. The samples stored at 60º C presented high peroxide index values, even though a minor improvement in the oxidative stability was noticed for the microencapsulated coffee oil in comparison with the pure one Mestrado Mestre em Engenharia de Alimentos

Agradecimentos: Ana Paula Badan Ribeiro thank Conselho Nacional de Desenvolvimento Científico e Tecnológico-CNPq, Brazil (grant number 303429/2018-6) for productivity grant and Fundação de Amparo à Pesquisa do Estado de São Paulo-FAPESP, Brazil (grant number 16/11261-8. Kamila Ramponi Rodrigues de Godoi thank Conselho Nacional de Desenvolvimento Científico e Tecnológico-CNPq, Brazil (grant number 140789/2017-0) for PhD scholarship grant. Lisandro Pavie Cardoso thank Conselho Nacional de Desenvolvimento Científico e Tecnológico-CNPq, Brazil (grant numbers 302626/2016-6 and 307896/2019-6) for productivity grant. This study was financed in part by the "Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - Brazil (CAPES)"–Finance Code 001 Abstract: The objective of this study was to develop new nanostructured lipid carrier (NLC) formulations loaded with free phytosterols (FPs) using interesterified and simple lipid phases. The simple and interesterified lipid phases were composed of soybean oil as liquid lipid and fully hydrogenated palm (HPO) and crambe (HCO) oils s solid lipids. High-pressure homogenization was the preparation method, with soy lecithin as a natural emulsifier. The characteristics of NLCs were influenced by chemical interesterification and the composition of solid lipid, mainly with respect to the fatty acid chain size. All developed FP-loaded NLCs displayed an appropriate nanoscale size from approximately 167 to 330 nm (d(32)) and appropriate physical stability with zeta potential values ranging from -29.83 to -43.70 mV after 30 days of storage. The changes observed in these parameters were influenced by the lipid phase of the NLCs and the crystallization of FP on the surface of the NLCs. FP-loaded NLCs formulated with interesterified blends displayed smaller particle size values, with less evidence of particle agglomeration and higher absolute zeta potential values than NLCs formulated with simple blends. These results indicated that NLCs developed with interesterified lipid blends were more stable than those developed with single blends NLCs produced from solid lipids with fatty acids with larger chain sizes (HCO) had larger particle sizes but were less likely to flocculate and coalesce. Thermal behavior study revealed that interesterification caused a reduction in the melting temperature and recrystallization index of the NLCs. These findings indicated decreased crystallinity and a less organized structure. This behavior favored the highest encapsulation efficiency and load capacity observed for NLCs developed with interesterified blends CONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQ FUNDAÇÃO DE AMPARO À PESQUISA DO ESTADO DE SÃO PAULO - FAPESP COORDENAÇÃO DE APERFEIÇOAMENTO DE PESSOAL DE NÍVEL SUPERIOR - CAPES Fechado

JOURNAL OF CURRENT SCIENCE AND TECHNOLOGY, 11, 1, 60-70

In recent years, starch nanoparticles (SNPs) have attracted growing attention due to their unique properties as a sustainable alternative to common nanomaterials since they are natural, renewable and biodegradable. SNPs can be obtained by the breakdown of starch granules through different techniques which include both physical and chemical methods. The final properties of the SNPs are strongly influenced by the synthesis method used as well as the operational conditions, where a controlled and monodispersed size is crucial for certain bioapplications. SNPs are considered to be a good vehicle to improve the controlled release of many bioactive compounds in different research fields due to their high biocompatibility, potential functionalization, and high surface/volume ratio. Their applications are frequently found in medicine, cosmetics, biotechnology, or the food industry, among others. Both the encapsulation properties as well as the releasing processes of the bioactive compounds are highly influenced by the size of the SNPs. In this review, a general description of the different types of SNPs (whole and hollow) synthesis methods is provided as well as on different techniques for encapsulating bioactive compounds, including direct and indirect methods, with application in several fields. Starches from different botanical sources and different bioactive compounds are compared with respect to the efficacy in vitro and in vivo. Applications and future research trends on SNPs synthesis have been included and discussed.

This review aims to provide an overview of polymers comprising cholesterol moiety/ies designed to be used in drug delivery. Over the last two decades, there have been many papers published in this field, which are summarized in this review. The primary focus of this article is on the methods of synthesis of polymers bearing cholesterol in the main chain or as side chains. The data related to the composition, molecular weight, and molecular weight distribution of polymers are presented. Moreover, other aspects, such as forms of carriers, types of encapsulated drugs, encapsulation efficiency and capacity, are also included.

PTDC/QEQEPR/5841/2014 PTDC/QEQ-FTT/3289/2014 IF/00210/2014/CP1244/CT0003 UIDB/50006/2020 Nowadays, pharmaceutical companies are facing several challenges with the development and approval of new biological products. The unique properties of several fluorinated ionic liquids (FILs), such as their high surfactant power in aqueous solutions, their chemical and biological stability, and low toxicity, favor their application in the pharmaceutical industry. Furthermore, the numerous combinations between cations and anions, in the FILs design, enlarge the possibilities to construct a successful delivery system. Several FILs also proved to not affect the activity, stability, and secondary structure of the therapeutic protein lysozyme. This work aims to study the aggregation behavior of distinct FILs in the protein suitable medium, in the presence or absence of lysozyme. Besides, different incubation conditions were tested to guarantee the optimal enzymatic activity of the protein at more stable delivery systems. Following the optimization of the incubation conditions, the quantification of the encapsulated lysozyme was performed to evaluate the encapsulation efficiency of each FIL-based system. The release of the protein was tested applying variables such as time, temperature, and ultrasound frequency. The experimental results suggest that the aggregation behavior of FILs is not significantly influenced by the protein and/or protein buffer and supports their application for the design of delivery systems with high encapsulation efficiencies, maintaining the biological activity of either encapsulated and released protein. publishersversion published

The evaluation of encapsulation efficiency is a regulatory requirement for the characterization of drug delivery systems. However, the difficulties in efficiently separating nanomedicines from the free drug may compromise the achievement of accurate determinations. Herein, ultrafiltration was exploited as a separative strategy towards the evaluation of methotrexate (MTX) encapsulation efficiency in nanostructured lipid carriers and polymeric nanoparticles. The effect of experimental conditions such as pH and the amount of surfactant present in the ultrafiltration media was addressed aiming at the selection of suitable conditions for the effective purification of nanocarriers. MTX-loaded nanoparticles were then submitted to ultrafiltration and the portions remaining in the upper compartment of the filtering device and in the ultrafiltrate were collected and analyzed by HPLC-UV using a reversed-phase (C18) monolithic column. A short centrifugation time (5 min) was suitable for establishing the amount of encapsulated MTX in nanostructured lipid carriers, based on the assumption that the free MTX concentration was the same in the upper compartment and in the ultrafiltrate. The defined conditions allowed the efficient separation of nanocarriers from the free drug, with recoveries of &gt, 85% even when nanoparticles were present in cell culture media and in pig skin surrogate from permeation assays.

Fragrances are widely used in our daily lives and can make us feel happy. However, traditional aromatic products release fragrance quickly and have a strong aroma. This not only worsens our scenting experience, but also severely shortens the useful life of fragrance products. In this study, nano‐fragrances based on mesoporous silica nanoparticles with great encapsulation efficiency and slow‐release function were designed and prepared. In addition, this nano‐fragrances are applied to wallpapers. Open field tests showed that this nano‐fragrance had significant stress relief and anti‐depressant effects.

Numerous attempts to overcome the poor water solubility of cam ptothecin (CPT) by various nano drug delivery systems are described in various sources in the literature. However, the results of these approaches may be hampered by the incomplete separation of free CPT from the formulations, and this issue has not been investigated in detail. This study aimed to promote the solubility and continuous delivery of CPT by developing long-lasting liposomes using various weights (M.W. 2000 and 5000 Daltons) of the hydrophilic polymer polyethylene glycol (PEG). Conventional and PEGylated liposomes containing CPT were formulated via the lipid film hydration method (solvent evaporation) using a rotary flash evaporator after optimising various formulation parameters. The following physicochemical characteristics were investigated: surface morphology, particle size, encapsulation efficiency, in vitro release, and formulation stability. Different molecular weights of PEG were used to improve the encapsulation efficiency and particle size. The stealth liposomes prepared with PEG5000 were discrete in shape and with a higher encapsulation efficiency (83 ± 0.4%) and a prolonged rate of drug release (32.2% in 9 h) compared with conventional liposomes (64.8 ± 0.8% and 52.4%, respectively) and stealth liposomes containing PEG2000 (79.00 ± 0.4% and 45.3%, respectively). Furthermore, the stealth liposomes prepared with PEG5000 were highly stable at refrigeration temperature. Significant changes were observed using various pharmacokinetic parameters (mean residence time (MRT), half-life, elimination rate, volume of distribution, clearance, and area under the curve) of stealth liposomes containing PEG2000 and PEG5000 compared with conventional liposomes. The stealth liposomes prepared with PEG5000 showed promising results with a slow rate of release over a long period compared with conventional liposomes and liposomes prepared with PEG2000, with altered tissue distribution and pharmacokinetic parameters.

Purpose: Biopharmaceutics classification system (BCS) class IV compounds, exhibits least oral bioavailability, low solubility and intestinal permeability among all pharmaceutical classes of drugs. Thus, these drugs need more compatible and efficient delivery system. Since, their solubility in various medium, remains a limitation so, polymeric nano coacervates based drug loading with modified approach for them may prove to be a solution ahead. Therefore, in present study Chitosan is opted for encapsulating the BCS class IV drug (Hydrochlorothiazide) to attain better stability, enhanced permeability and lower toxicity. Methods: For this study, Hydrochlorothiazide (HCTZ) was opted for formulating chitosan based nano-coacervate system. Results: Optimized HCTZ nanocoacervates exhibited the average particle size of 91.39 ± 0.75 nm with Poly-dispersity index score of 0.159 ± 0.01, indicating homogeneity of colloidal solution. Zeta potential and encapsulation efficiency of HCTZ nanocoacervates were recorded as -18.9 ± 0.8 mV and 76.69 ± 0.82 % respectively. Further, from TEM and SEM evaluation the average particle size for the same were found in conformity (35-50 nm), with almost spherical morphology. Also, the EDX (Electron Dispersive X-ray) spectrometry and FT – IR analysis of optimized formulation indicated the balanced chemical composition and interaction between the polymeric molecules. The HCTZ nano coacervates showed the linear diffusion profile through the dialysis membrane. Conclusion: We can conclude from the present study that the optimized HCTZ nano coacervates may prove to be a suitable potential option for effective delivery of BCS class IV drugs.

A strategic pathway in creating high-potent medical products is with targeted therapeutic systems that are based on nanoparticles of various structure. Such particles are capable of providing a targeted effect and an increase in bioavailability of the medical products. A special place among modern targeted drug delivery systems is held by liposomal nanoparticles which have apparent advantages over nanoparticles of an another type The problem number one for pharmacy lies in developing specific methods of control of nanosize drug delivery systems. This research is dedicated to the development and validation of a technique for determining encapsulation efficiency of cytochrome C in liposomes. The subject of research comprised the obtained liposomal form of cytochrome C, placebo emulsion, and cytochrome C solution. The research was conducted in compliance with the ICH and FDA requirements and recommendations in relation to the development of HPLC methods of control of liposomal preparations. A method has been developed to enable the determination of encapsulation efficiency of cytochrome C in liposomal preparations and to allow for identifying the composition of liposomal nanoparticles of cytochrome C. This HPLC method has been validated in terms of specificity, limit of detection, and robustness in compliance with the recommended criteria. The technique may find its application in quality control of liposomal form of cytochrome C and in control points manufacturing process.

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. This is the peer-reviewed version of the article: Jovanović, Miloš, Ćujić-Nikolić, Nada, Drinić, Zorica, Janković, Teodora, Marković, Smilja, Petrović, Predrag, Šavikin, Katarina, "Spray drying of Gentiana asclepiadea L. root extract: Successful encapsulation into powders with preserved stability of bioactive compounds" in Industrial Crops and Products, 172 (2021):114044, [https://doi.org/10.1016/j.indcrop.2021.114044]

[EN] Carvacrol (CA) was encapsulated in polar (corn starch-Sodium caseinate, CS:NaCas) or non-polar (poly-¿-caprolactone, PCL) matrices by electrospinning (ES). Electrospunable formulations were prepared with CS:NaCas (9:1 w/w ratio), at 2, 4 and 6 wt % in water, or PCL at 5, 10 and 15 wt% in glacial acetic acid using different CA ratios (0, 5, 10 and 15 wt% with respect to the polymer). The liquid formulations were characterized for electrical conductivity, rheological behaviour and surface tension, and ES process conditions were established. The electrospun structures were analysed as to their nanostructure and CA retention. Geometry of the nanostructures obtained from the PCL systems was nanofibrillar with some beads, whereas it is particles that are mainly deposited for starch systems. PCL systems yielded better CA encapsulation efficiency (EE) than the polar ones, where greater variability was observed. The best EE (around 80%) was obtained for 15% PCL regardless of the CA ratio., The authors would like to thank the Ministerio de Economia y Competitividad of Spain, for funding this study as part of projects AGL2013-42989-R and AGL2016-76699-R and predoctoral research grant # BES-2014-068100.

Made available in DSpace on 2018-12-11T16:50:58Z (GMT). No. of bitstreams: 0 Previous issue date: 2017-12-29 Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) The influence of hydrodynamic conditions in the coacervation medium of the carotenoid-rich buriti oil using gelatin-alginate as wall materials was investigated. The stirring speed had strong influence on the size of the microcapsules, and Reynolds number higher than 70000 resulted in particle size D[4,3] lower than 200 μm. The carotenoid encapsulation efficiency was around 80%, with freeze-dried particles presenting intense yellow color. Although the size of the microparticles was highly dependent on the hydrodynamic conditions during coacervate formation, complex coacervation of gelatin and sodium alginate showed to be a feasible process to producing buriti oil microcapsules. UNESP - Universidade Estadual Paulista Júlio de Mesquita Filho Departamento de Engenharia e Tecnologia de Alimentos Universidade Federal do Triângulo Mineiro Departamento de Engenharia de Alimentos UNESP - Universidade Estadual Paulista Júlio de Mesquita Filho Departamento de Engenharia e Tecnologia de Alimentos FAPESP: 2014/02910-7

The aim of this study is to formulate and characterize streptomycin-loaded apoferritin nanoparticles ( ApoStrep NPs ) for their potential therapeutic use in bacterial resistant infections (i.e. tuberculosis). ApoStrep NPs were prepared by disassembly/reassembly process via pH method and changing apoferritin/drug molar ratio, purified by dialyses process also associated with gel filtration chromatography and characterized in their chemico-physical and technological parameters as yield, size distribution, polidispersivity, morphology, internal structure, zeta potential and loading efficacy. The results showed that spherical reproducible NPs could be obtained by using apoferritin/drug molar ratio lower than 1:25 and purification based on the combination of dialysis and gel filtration chromatography. Photon correlation spectroscopy, Uv–visible detection and electron microscopy showed the maintenance of the native apoferritin chemico-physical properties and structure. When formulated with apoferritin/drug 1:10 and 1:25 molar ratio, ApoStrep NPs showed remarkable encapsulation efficacy (35% and 28%, respectively) along with kinetic profile of drug delivery, approximately 15% at 37 °C in 72 h, as evidenced by “in vitro” release experiments.

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., This work was supported by Spanish Government (FORCHRONIC Project: ALG-2016-76736-C3-1-R), by Comunidad Autónoma de Madrid (ALIBIRD project: P2018/BAA-4343) and by the Natural Sciences and Engineering Council of Canada, through the Canada Research Chair programme.

Polyurea, a controlled release material, has been widely applied in agricultural fields due to high thermal stability and low cost. In this article oxyfluorfen polyurea microcapsules suspension was successfully prepared by interfacial polymerization using diisocyanate and polyamines such as Ethylenediamine, Hexamethylenediamine, Diethylenetriamine in presence of green solvent, i.e., N,N-dimethyldecanamide. The microcapsule suspension of oxyfluorfen has not been researched yet by using solvent N,N-dimethyldecanamide and polyamines. The effect and the type of diamines on the morphology and properties of the microcapsules have been investigated. The synthesized microcapsules were characterized by scanning electron microscope, ultraviolet spectrometry, Fourier transform iInfrared spectrometer, thermogravimetric analysis and particle size analyser. The effect of the core to shell ratio on encapsulation efficiency and release kinetics were also studied. The oxyfluorfen microcapsules had an excellent encapsulation efficiency (98.2%) using EDA as the monomer and Release kinetics depended upon the type of monomers used and also on core to shell ratio used (6.5:1, 5:1, 4:1). As core to shell ratio was increased the encapsulation efficiency was found to decrease. Prepared Microcapsules when sprayed on paddy crop was found to be safe in comparison with Emulsifiable concentrate sample.

Vesicular nanocarriers have an important role in drug delivery and dietary supplements. Size control and optimization of encapsulation efficiency (EE) should be optimized for those applications. In this work, we report on the identification of the crucial step (injection, evaporation, or sonication) innanovesicles (transfersomes and niosomes) preparation by theethanol injection method (EI). The identification of each production step on the final vesicle size was analyzed in order to optimize further scale-up process. Results indicated that the final size of transfersomeswas clearly influenced by the sonication step while the final size of niosomes was mainly governed by the injection step. Measurements of final surface tension of the different vesicular systems prepared indicate a linear positive tendency with the vesicle size formed. This relation could help to better understand the process and design a vesicular size prediction model for EI. Vitamin D3 (VitD3) was encapsulated in the systems formulated with encapsulation efficiencies larger than 90%. Interaction between the encapsulated compound and the membrane layer components is crucial for vesicle stability. This work has an impact on the scaling-up production of vesicles for further food science applications.

The dataset presents the synthesis and physicochemical characterization of blank and curcumin encapsulated sericin protein nanoparticles obtained from Philosamia ricini (also known as Ahimsa silk or Peace silk or Eri). Reports on application of sericin protein obtained from P. ricini are scanty at best. Sericin was extracted from the cocoons by high temperature and high pressure method. Synthesis of sericin nanoparticles was carried out by desolvation method using acetone as the desolvating agent. Curcumin was used as a hydrophobic model drug and was encapsulated into the sericin nanoparticles. Physicochemical characterization of the blank and curcumin encapsulated sericin nanoparticles were carried out by different instrumental analyses. The size and surface charges of sericin nanoparticles changed with the variation of applied sericin concentration. Encapsulation efficiency and loading capacity of the encapsulated sericin nanoparticles showed variation with curcumin concentration. The obtained data indicated the applicative potentials of sericin protein extracted from Philosamia ricini silkworm cocoons.

Background and aim Methicillin-resistant Staphylococcus aureus (MRSA) is one of the most common causes of surgical infection, and its resistance to numerous conventional antibiotics makes treatment difficult. Although vancomycin is often an effective agent for the initial therapy of MRSA, clinical failure sometimes occurs. Therefore, there is an urgent need to develop better therapies. Here, we prepared some vancomycin-loaded nanoliposomes coupled with anti-staphylococcal protein (lysostaphin) and evaluated their in vitro and in vivo efficacy as a topical MRSA therapy. Methods Vancomycin was encapsulated in liposomes, and the coupling of lysostaphin with the surface of liposomes was carried out through cyanuric functional groups. The bactericidal efficacies and a full characterization were evaluated. To define different nanoliposomal–bacterium interactions and their bactericidal effect, flow cytometry was employed. Finally, in vivo, the topical antibacterial activity of each formulation was measured against surgical wound MRSA infection in a mouse model. Results High encapsulation and conjugation efficiency were achieved for all formulations. All the formulations showed a significant reduction in bacterial counts (p

Two multi-functional powders, in terms of anthocyanins from black rice (Oryza sativa L.) and lactic acid bacteria (Lactobacillus paracasei, L. casei 431®) were obtained through co-microencapsulation into a biopolymer matrix composed of milk proteins and inulin. Two extracts were obtained using black rice flour as a raw material and hot water and ethanol as solvents. Both powders (called P1 for aqueous extract and P2 for ethanolic extract) proved to be rich sources of valuable bioactives, with microencapsulation efficiency up to 80%, both for anthocyanins and lactic acid bacteria. A higher content of anthocyanins was found in P1, of 102.91 ± 1.83 mg cyanindin-3-O-glucoside (C3G)/g dry weight (DW) when compared with only 27.60 ± 17.36 mg C3G/g DW in P2. The morphological analysis revealed the presence of large, thin, and fragile structures, with different sizes. A different pattern of gastric digestion was observed, with a highly protective effect of the matrix in P1 and a maximum decrease in anthocyanins of approximatively 44% in P2. In intestinal juice, the anthocyanins decreased significantly in P2, reaching a maximum of 97% at the end of digestion, whereas in P1, more than 45% from the initial anthocyanins content remained in the microparticles. Overall, the short-term storage stability test revealed a release of bioactive from P2 and a decrease in P1. The viable cells of lactic acid bacteria after 21 days of storage reached 7 log colony forming units (CFU)/g DW.

Apigenin (Apig) is used as a model drug due to its many beneficial bio-activities and therapeutic potentials. Nevertheless, its poor water solubility and low storage stability have limited its application feasibility on the pharmaceutical field. To address this issue, this study developed nanoemulsions (NEs) using an anti-oxidative polymeric amphiphile, d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), hydrogenated soy lecithin (HL), black soldier fly larvae (BSFL) oil, and avocado (AV) oil through pre-homogenization and ultrasonication method. Addition of TPGS (weight ratios 100 and 50% as compared to HL) into NEs effectively reduced particle size and phase transition region area of NEs with pure HL. Incorporation of Apig into NEs made particle size increase and provided a disorder effect on intraparticle molecular packing. Nevertheless, the encapsulation efficiency of NEs for Apig approached to about 99%. The chemical stability of Apig was significantly improved and its antioxidant ability was elevated by incorporation with BSFL oil and AV oil NEs, especially for NEs with single TPGS. NEs with single TPGS also exhibited the best Apig skin deposition. For future application of topical Apig delivery, NEs-gel was formed by the addition of hyaluronic acid (HA) into NEs. Their rheological characteristics were dominated by the surfactant ratios of HL to TPGS.

Made available in DSpace on 2021-06-25T10:14:41Z (GMT). No. of bitstreams: 0 Previous issue date: 2020-12-01 This study investigates the influence of the atomization parameters on complex coacervation by atomization, and is following a preceding study that presented the technique and investigated the effects of formulation. Complex coacervated capsules were produced by atomization, using emulsions with 1 and 6%(w/w) of gelatin and ginger oil atomized over a 1%(w/w) solution of gum Arabic, at constant polymer ratio of 1:2 (gelatin:gum Arabic) at pH 3.5. The air velocity at the nozzle varied from 72 to 168 m/s and the emulsion velocity at the nozzle varied from 0.4 to 0.6 m/s, maintaining the air to liquid velocity ratio at 170, 220 and 270. The mean diameter of the microcapsules produced varied from 52 to 75 μm and no crosslinking agents were used. The influence of atomization numbers Weber (We) and Ohnesorge (Oh), shear rate and shear stress on the encapsulation performance was carried out and a proposed model was able to predict the final size of the microcapsules produced at We ≥ 180 and Oh = 0.063. Encapsulation efficiency varied from 9 to 95%, and encapsulation yield varied from 50 to 99%. Finally, optimum conditions based on size prediction and microencapsulation parameters were proposed. São Paulo State University (UNESP) Department of Food Engineering and Technology São Paulo State University (UNESP) Department of Food Engineering and Technology

[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, The authors thank the Ministerio de Economia y Competitividad (MINECO) of Spain, for the financial support provided for this study as part of the project AGL2016-76699-R. The author A. Tampau also thanks MINECO for the pre-doctoral research grant #BES-2014068100

Droplet-based microfluidics offers significant advantages, such as high throughput and scalability, making platforms based on this technology ideal candidates for point-of-care (POC) testing and clinical diagnosis. However, the efficiency of co-encapsulation in droplets is suboptimal, limiting the applicability of such platforms for the biosensing applications. The homogeneity of the bioanalytes in the droplets is an unsolved problem. While there is extensive literature on the experimental setups and active methods used to increase the efficiency of such platforms, passive techniques have received less attention, and their fundamentals have not been fully explored. Here, we develop a novel passive technique for investigating cell encapsulation using the finite element method (FEM). The level set method was used to track the interfaces of forming droplets. The effects of walls and the droplet interfaces on relatively large cells were calculated to track them more accurately during encapsulation. The static surface tension force was used to account for the effects of the interfaces on cells. The results revealed that the pairing efficiency is highly sensitive to the standard deviation (SD) of the distance between the cells in the entrance channel. The pairing efficiency prediction error of our model differed by less than 5% from previous experiments. The proposed model can be used to evaluate the performance of droplet-based microfluidic devices to ensure higher precision for co-encapsulation of cells.

Highly concentrated (HC) emulsions and or submicron emulsions arise as an interesting strategy to encapsulate and transport labile lipophilic bioactive compounds such as curcumin to be further incorporated into food formulations. The main factors affecting HC-emulsions formation and stabilization are the homogenization process, the oil volume fraction (phi) and the surfactant to oil ratio (SOR). Therefore, different HC emulsions were prepared by high-shear homogenization (HSH; 11,000 rpm, 2 min), ultrasonication (US; 100 mu m, 20-300 s) or microfluidization (MF; 800 bar, 1-5 cycles) varying the phi from 0.4 to 0.7 (40%-70% w/w) and the SOR from 0.01 to 0.2. HSH led to HC emulsions, whose particle sizes decreased from 14.46 to 2.42 mu m (d(43)), as the phi increased from 0.4 to 0.7. However, US and MF provoked the droplet breakup at oil concentrations over 50% w/w. Additionally, the higher the SOR at a fixed phi, the smaller the particle size of the resultant HC emulsions regardless the homogenization procedure applied. Overall, particle size reduction produced a dramatic increase in emulsion viscosity due to a high packing state of droplets that in turn prevented droplets re-coalescence. Moreover, HC emulsions presented a high curcumin encapsulation efficiency (> 70%) and release (> 80% after 48 h is). Therefore, this work contributes to demonstrate that the small droplets size is governing the apparent viscosity in HC systems, as well as to elucidate the factors affecting their formation to be used as potential carriers of lipophilic bioactive compounds. This study was funded by the Ministry of Economy, Industry and Competitiveness (MINECO/FEDER, UE) throughout project AGL2015-65975-R. María Artiga-Artigas thanks the University of Lleida for her pre-doctoral fellowship. Laura Salvia-Trujillo thanks the “Secretaria d’Universitats i Recerca del Departament d’Empresa i Coneixement de la Generalitat de Catalunya” for the Beatriu de Pinós post-doctoral grant (BdP2016-00336).

Purple flesh cultivated potato (PP) is a foodstuff scarcely cultivated in the world but with high potential because of its anthocyanin content. Moreover, it has been little explored as a source of anthocyanins (AT) for further applications in formulated food products. The main goal of this research was to study the effect of maltodextrin (MD) and spray drying conditions on the encapsulation efficiency (EE) and bioaccesibility of AT from purple flesh cultivated potato extract (PPE). The anthocyanin-rich extract was obtained from PP and microencapsulated by spray-drying, using MD as the encapsulating agent. A statistical optimization approach was used to obtain optimal microencapsulation conditions. The PPE microparticles obtained under optimal conditions showed 86% of EE. The protector effect of microencapsulation on AT was observed to be stable during storage and in vitro digestion. The AT degradation rate constant was significantly lower for the PPE-MD than for the PPE. The assessed bioaccesibility of AT from the PPE-MD was 20% higher than that of the PPE, which could be explained by the protective effect of encapsulation against environmental conditions. In conclusion, microencapsulation is an effective strategy to protect AT from PP, suggesting that AT may be an alternative as a stable colorant for use in the food industry.

In this study, daidzein long-circulating liposomes (DLCL) were prepared using the ultrasonication and lipid film-hydration method. The optimized preparation conditions by the orthogonal design was as follows: 55 to 40 for the molar ratio of soybean phosphatidylcholine (SPC) to cholesterol, 1 to 10 for the mass ratio of daidzein to total lipid (SPC and cholesterol) (w:w), the indicated concentration of 5% DSPE-mPEG2000 (w:w), 50 °C for the hydration temperature, and 24 min for the ultrasonic time. Under these conditions, the encapsulation efficiency and drug loading of DLCL were 85.3 ± 3.6% and 8.2 ± 1.4%, respectively. The complete release times of DLCL in the medium of pH 1.2 and pH 6.9 increased by four- and twofold of that of free drugs, respectively. After rats were orally administered, a single dose of daidzein (30 mg/kg) and DLCL (containing equal dose of daidzein), respectively, and the MRT0−t (mean residence time, which is the time required for the elimination of 63.2% of drug in the body), t1/2 (the elimination half-life, which is the time required to halve the plasma drug concentration of the terminal phase), and AUC0−t (the area under the plasma drug concentration-time curve, which represents the total absorption after a single dose and reflects the drug absorption degree) of daidzein in DLCL group, increased by 1.6-, 1.8- and 2.5-fold as compared with those in the free group daidzein. Our results indicated that DLCL could not only reduce the first-pass effect of daidzein to promote its oral absorption, but also prolong its mean resident time to achieve the slow-release effect.

[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., This work was supported by a grant for Annika Linke from the Ministry of Science, Research and the Arts of Baden-Württemberg (MWK) Az: 7533-10-5-87. Furthermore, the author acknowledges generous support by the bioeconomy graduate program BBW ForWerts, supported by the MWK

We report a simple strategy to prepare Tween 60@2β-CD self-assembly vesicles in aqueous solution as a new drug delivery carrier for cancer chemotherapy. The spherical shape of vesicles was confirmed by transmission electron microscopy (TEM) and mean particle sizes were about 33.7 nm, as measured by dynamic light scattering, micro-IR results indicated that the self-assembly vesicles was driven by hydrogen bonding. Hydrophilic doxorubicin (DOX) was successfully loaded into the self-assembly vesicles with drug loading content of 7.85% and loading efficiency of 42%. In addition, an in vitro cytotoxicity study and cellular uptake assays demonstrated that the DOX-loaded Tween 60@2β-CD vesicles markedly enhanced the cellular uptake and cytotoxicity of DOX toward the Hela cells. Furthermore, when used to evaluate the in vivo therapeutic efficacy in mice bearing the breast cell line (4T1), DOX-loaded vesicles exhibited superior inhibition of tumor growth compared with the DOX solutions.

Tuberculosis (TB) is still a devastating disease and more people have died of TB than any other infectious diseases throughout the history. The current therapy consists of a multidrug combination in a long-term treatment, being associated with the appearance of several adverse effects. Thus, solid lipid nanoparticles (SLNs) were developed using mannose as a lectin receptor ligand conjugate for macrophage targeting and to increase the therapeutic index of rifampicin (RIF). The developed SLNs were studied in terms of diameter, polydispersity index, zeta potential, encapsulation efficiency (EE) and loading capacity (LC). Morphology, in vitro drug release and differential scanning calorimetry studies, macrophage uptake studies, cell viability and storage stability studies were also performed. The diameter of the SLNs obtained was within the range of 160–250 nm and drug EE was above 75%. The biocompatibility of M-SLNs was verified and the internalization in macrophages was improved with the mannosylation. The overall results suggested that the developed mannosylated formulations are safe and a promising tool for TB therapy targeted for macrophages. The authors also thank the CNPq Foundation, Ministry of Education of Brazil for the Doctoral fellowship 246514/2012–4 and FCT for the PostDoctoral fellowship SFRH/BPD/99124/2013. SCL thanks Operac¸ão NORTE-01–0145-FEDER-000011 for her investigator contract. This work received financial support from the European Union (FEDER funds) and National Funds [FCT/MEC, Fundac¸ão para a Ciência e Tecnologia and Ministério da Educac¸ão e Ciência] under the Partnership Agreement PT2020 UID/MULTI/04378/2013 – POCI/01/0145/FEDER/ 007728. This work was financed by FEDER – Fundo Europeu de Desenvolvimento Regional funds through the COMPETE 2020 – Operational Programme for Competitiveness and Internationalisation (POCI), Portugal 2020 [NORTE-01–0145-FEDER-000012], and by Portuguese funds through FCT – Fundac¸ão para a Ciência e a Tecnologia/Ministério da Ciência, Tecnologia e Inovac¸ão in the framework of the project “Institute for Research and Innovation in Health Sciences” [POCI-01–0145-FEDER-007274].