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Curcumin, is the main bioactive component of temulawak (Curcuma xanthorriza Roxb), which is a native Indonesian herbal plant. Although it has various health benefits, curcumin's stability and release time are very low, limiting its application. This study aimed to improve curcumin stability through spray-drying microencapsulation using various wall materials, including maltodextrin (MDE), gum Arabic (GAR), whey protein isolate (WPI), and their composites with ß-cyclodextrin (ßCD). The resulting curcumin microcapsules from temulawak extract had an irregular morphology with a rough surface and grooves, averaging 2 µm in diameter. The stability of curcumin during storage, against heat and various pH conditions increased significantly, especially in microcapsules prepared with composite wall materials. Curcumin release was faster in single wall material microcapsules, while composite wall material microcapsules achieved release times over 120 min. In conclusion, curcumin from temulawak extract can be prepared by spray drying. MDE-ßCD composite wall materials are highly recommended because they produce curcumin microcapsules with improved stability and controlled release compared to single wall materials or other composite wall materials. This research can facilitate the utilization of curcumin from temulawak extract in industrial and food applications. [ABSTRACT FROM AUTHOR]

This work evaluates the effectiveness of coating bronze coupons, with 3% Benzotriazole (BTA) -loaded nanocontainers mixed with Paraloid polymer. Mesoporous silica nanoparticles (MSNs) were prepared and loaded with 3% BTA (BTA@MSNs) followed by dispersion in 3% Paraloid B72 and B44. Bronze disc samples with the chemical composition of Cu 85%, Sn 10% and Pb 5% simulating archaeological artifacts were coated with a single and double layer of BTA@MSNs in Paraloid B72 and B44 and evaluated using several techniques. Colorimetric measurements (CM) were used to evaluate changes in the surface appearance following the coating with single and double protective layers. The corrosion inhibitive performance of the coating was investigated using electrochemical impedance spectroscopy (EIS). Transmission electron microscope (TEM) was performed to characterize the shape and size of the prepared SiO2 nanoparticles, while X-ray Diffraction (XRD) was performed to confirm the presence of amorphous mesoporous SiO2 nanoparticles. The specific surface area, pore volume and pore size distribution were measured by nitrogen adsorption-desorption technique, while the release rate of benzotriazole at various experimental pH values was estimated using UV-Vis spectroscopy. Results confirmed the sustained release of benzotriazole to varying pH levels. The release was higher with an increase in the pH of the medium, which signifies that the release rate rises in the alkaline medium. The best corrosion inhibitive performance was for the double layer BTA@MSNs - B72 samples at 91.73% efficiency, while single layer BTA@MSNs - B72 samples displayed the least change in color ΔE 3.28. [ABSTRACT FROM AUTHOR]

The aim of this study was to assess the impact of physiological factors, namely tear fluid and lysozyme enzyme, as well as surfactant polysorbate, on the release profile from solid lipid microparticles (SLM), in the form of dispersion intended for ocular application. Indomethacin (Ind) was used as a model drug substance and a release study was performed by applying the dialysis bag method. Conducting release studies taking into account physiological factors is expected to improve development and screening studies, as well as support the regulatory assessment of this multi-compartment lipid dosage form. The effect of the lysozyme was directly related to its effect on lipid microparticles, as it occurred only in their presence (no effect on the solubility of Ind). Polysorbate also turned out to be an important factor interacting with the SLM surface, which determined the release of Ind from SLM. However, in study models without tear fluid or lysozyme, the release of Ind did not exceed 60% within 96 h. Ultimately, only the simultaneous application of artificial tear fluid, lysozyme, and polysorbate allowed for the release of 100% of Ind through the SLM dispersion. The examination of the residues after the release studies indicated the possibility of releasing 100% of Ind from SLM without complete degradation of the microparticles' matrix. The incubation of SLM with tear fluid confirmed a similar influence of physiological factors contained in tear fluid on the surface structure of SLM as that observed during the in vitro studies. [ABSTRACT FROM AUTHOR]

In the present study, extraction of nutraceuticals from neem leaves (Azadirachta indica A. Juss) was optimized using different extraction methods and solvents. Nutraceuticals possessing antimicrobial activities has been studied. The maximum amount of yield of neem oil was obtained when methanol was used and the yield comes out to be 7.68±0.11% by weight. 100 µL of extracted neem oil was incorporated in three different types of hydrogels of different proportions such as Chitosan-Gelatin hydrogel (1:1. 1.67:1 and 1:5), Maltodextrin-Whey protein (1:2) and Gum Arabic hydrogel and the release behavior was determined. The neem nutraceutical release was maximum (89.99 %) in case of Chitosan-Gelatin hydrogel where chitosan and gelatin was in the ratio of 5:1 and the amount of nutraceutical present was 100 µL, whereas the amount of drug release was observed minimum (44.45 %) in Gum Arabic hydrogel.

Infected burned skin is a life-threatening condition, which may lead to sepsis. The aims of this work are to formulate a biofilm composed of silver sulfadiazine (SSD), chitosan (CS), and sodium alginate (SA), and to evaluate its wound-healing effectiveness. A full factorial design was used to formulate different matrix formulations. The prepared biofilm was tested for physicochemical, and in vitro release. The optimized formulation is composed of 0.833% of CS and 0.75% of SA. The release of SSD almost reached 100% after 6 h. The mechanical properties of the optimized formula were reasonable. The antibacterial activity for the optimized biofilm was significantly higher than that of blank biofilm, which is composed of CS and SA, p = 1.53922 × 10−12. Moreover, the in vivo study showed a 75% reduction in wound width when using the formulated SSD biofilm compared to standard marketed cream (57%) and the untreated group (0%). [ABSTRACT FROM AUTHOR]

Curcumin, a molecule with medicinal properties, has been encapsulated in alginate microbeads through the ion gelation method. The size of the microbeads were 500-700 microns and stable under normal condition. FTIR and thermal analysis suggested that curcumin was successfully loaded in the microbeads. 110 mg of curcumin was loaded per gram of dry weight of microbeads, whereas the encapsulation efficiency was 71%. Curcumin release from these microbeads was studied in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The release of curcumin was higher and faster in SIF compared to SGF. Higher swelling of microbeads in SIF was responsible for this release behaviour. The absorption of the food particles mostly occurs in the intestinal region, and these microbeads easily travel through the gastric region without much degradation. Curcumin suffers degradation via auto-oxidation in the biological medium; thus, the release of curcumin in the intestinal region will help its maximum absorption. Curcumin was encapsulated in alginate microbeads through the ion gelation method. The size of the microbeads was 500-700 microns. Curcumin release from these microbeads was considerably less in simulated gastric fluid (SGF) than simulated intestinal fluid (SIF) and thus facilitated maximum absorption of curcumin in the intestinal region. [ABSTRACT FROM AUTHOR]

Herbicides based formulations are conventionally used as wettable powder or as Emulsifiable concentrate. The Emulsifiable Concentrates (EC) are prepared by mixing the active content with solvents and surfactants. However, these formulations have undesirable phytotoxic effects due to hazardous solvent and are unsafe to operators during application. Thus, capsule suspension (CS) formulation is considered as an alternative to EC formulations. In this study, we report the preparation of CS formulation of herbicide oxyfluorfen by polymerizing Methylene diphenyldiisocyanate (MDI) and Ethylenediamine (EDA). Water suspensions of the oxyfluorfen microcapsules were prepared by adding anionic, nonionic, polymeric surfactants and formulation auxiliaries. The study also aimed to determine the effect of surfactant on the stability of the microcapsule suspension. It was found that the nature of surfactant influenced the properties of the formulation. The synthesized microcapsules were characterized by Scanning electron microscope (SEM), Fourier Transform Infrared (FTIR) spectroscopy and thermogravimetric analysis (TGA). The microcapsule suspensions were applied on rice crop to establish the safety and its future use instead of oxyfluorfen EC. [ABSTRACT FROM AUTHOR]

The release profiles of active substances from microspheres are one of the most important features in solid lipid microparticles (SLM) characterization. Unfortunately, the results of the dissolution tests are largely dependent on the chosen method and test conditions, which in relation to novel dosage forms, such as dispersions of lipid microspheres, are not clearly defined in international compendiums and guidelines. This makes it impossible to compare the results of different studies. The aim of the research was to identify the factors most influencing the variability of the obtained results. An attempt was also made to select the most appropriate method for testing drug substance release from SLM. Various dissolution methods were employed (method I: without a membrane, method II: in a dialysis bag, and method III: in a Side-Bi-Side chamber), and the obtained release profiles of cyclosporine and indomethacin from SLM dispersions were compared. In addition to the effect of membranes, the types of acceptor fluids were also investigated. Significant differences were observed when testing the SLM formulations under various test conditions. The results were significantly influenced by the selected membrane, the acceptor fluid, or the difference in the concentrations of active substance between the donor and acceptor compartments. The burst effect observed in some experimental methods was not noticed in other conditions. At this stage, the method with a dialysis bag has been selected as the most suitable, while the methods without the membrane can only play a complementary role. [ABSTRACT FROM AUTHOR]

The problem of drug delivery often concentrates on the prolongation of drug activity. Application of natural polymers which are biodegradable and inexpensive is in the interest of many researchers. The aim of this study was the application of newly synthesized starch derivatives as potential functional excipients proposed for hydrophilic gel with lidocaine hydrochloride (LH) to prolong drug release from the hydrogel matrix. In our study, we investigated the effect of starch modified with citric acid on the release kinetics of LH using UV-VIS and Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), as well as viscosity and pH measurements. We demonstrated the effectiveness of citric-acid-modified starch in prolonging the release of LH from methylcellulose gel. [ABSTRACT FROM AUTHOR]

Infected burned skin is a life-threatening condition, which may lead to sepsis. The aims of this work are to formulate a biofilm composed of silver sulfadiazine (SSD), chitosan (CS), and sodium alginate (SA), and to evaluate its wound-healing effectiveness. A full factorial design was used to formulate different matrix formulations. The prepared biofilm was tested for physicochemical, and in vitro release. The optimized formulation is composed of 0.833% of CS and 0.75% of SA. The release of SSD almost reached 100% after 6 h. The mechanical properties of the optimized formula were reasonable. The antibacterial activity for the optimized biofilm was significantly higher than that of blank biofilm, which is composed of CS and SA, p = 1.53922 × 10−12. Moreover, the in vivo study showed a 75% reduction in wound width when using the formulated SSD biofilm compared to standard marketed cream (57%) and the untreated group (0%).

Extrusion is a common manufacturing process for semi-finished polymer products in various biomedical applications. Extrusion enables processing of a wide range of biomaterials, as well as different cross-sectional geometries. Furthermore, feasibility of drug elution, as it is used for a variety of medical devices, for example microstents for minimally invasive glaucoma therapy, was assessed. The current study deals with manufacturing of polymeric microtubes by extrusion processing. Semi-finished products were made of biodegradable poly-L-lactide (PLLA) and a non-biodegradable polycarbonate-based silicone elastomer (SIL) and covered with a polymer/drug combination, with resveratrol as active ingredient. Three different concentrations of polymer/resveratrol were applied by means of spray-coating. The release behavior of active ingredient was analyzed in vitro at 37°C and showed a correlation between the amount of drug and release time. With higher drug content, a faster release was observed. In addition, the release from SIL was faster compared with PLLA.

Fungal infections are very alarming nowadays and are common throughout the world. Severe fungal infections may lead to a significant risk of mortality and morbidity worldwide. Sustained delivery of antifungal agents is needed to mitigate this problem. In the current study, an attempt has been made to formulate griseofulvin-loaded nanosponges using the quasi-emulsion solvent diffusion technique. For characterization, griseofulvin loaded nanosponges were tested by different instrumental techniques such as optical microscopy, scanning electron microscopy (SEM), powder X-ray diffractometer (PXRD), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and transmission electron microscopy (TEM). The antifungal activity of the nanosponges was assessed against Candida albican strain using the agar well-diffusion method. Finally, the drug-loaded nanosponges' in vitro sustained release activity was evaluated. FTIR spectra showed no chemical interference between the drug and polymers. Some of the peaks of the drug are not visible in the FTIR spectrum, which suggests drug entrapment. PXRD data showed that the drug lost its high crystallinity when entrapped in the nanosponge matrix. From the morphological studies via SEM and TEM, a brief idea of the surface morphology of the nanosponges was obtained. The small pores throughout the structure proved its high porosity. The antifungal sensitivity assay was successful, and a zone of inhibition was observed in all the formulations. The in-vitro drug release study showed sustained behaviour. The sustaining effect was due to the polymer and cross-linker used, which gave rise to a porous scaffold matrix. From the results, it can be concluded that griseofulvin-loaded nanosponges can be used for antifungal drug delivery against various topical skin infections. [ABSTRACT FROM AUTHOR]

Ibuprofen is a non-steroidal, anti-inflammatory drug that is widely prescribed for its analgesic, antipyretic, and anti-inflammatory actions to treat pain, symptoms of rheumatoid arthritis and fever, but it is also known to cause stomach-related side effects. The development of efficient drug delivery systems for this compound to prevent these side effects is hampered by its poor water solubility. In this work, we show that graphite oxide and its derivatives have great potential as effective drug delivery systems not only to overcome side effects but also to increase the short biological half-life of ibuprofen. We studied the adsorption capacity of graphite oxide and carboxylated and sulfonated graphene oxide for this drug and its release in simulated gastric and intestinal fluid. The obtained compounds were characterized by X-ray diffraction, thermogravimetric analysis and Fourier transform infrared spectroscopy. DFT calculations were conducted to elucidate the Ibuprofen/host interactions, to establish which properties of these carbon nanomaterials control the loading and release, as well as to provide a better understanding of the orientation of the drug molecules on the single-layer GO. [ABSTRACT FROM AUTHOR]

Turmeric oil (TO) exhibits various biological activities with limited therapeutic applications due to its instability, volatility, and poor water solubility. Here, we encapsulated TO in chitosan/alginate nanocapsules (CS/Alg-NCs) using o/w emulsification to enhance its physicochemical characteristics, using poloxamer 407 as a non-ionic surfactant. TO-loaded CS/Alg-NCs (TO-CS/Alg-NCs) were prepared with satisfactory features, encapsulation efficiency, release characteristics, and cytotoxicity against breast cancer cells. The average size of the fabricated TO-CS/Alg-NCs was around 200 nm; their distribution was homogenous, and their shapes were spherical, with smooth surfaces. The TO-CS/Alg-NCs showed a high encapsulation efficiency, of 70%, with a sustained release of TO at approximately 50% after 12 h at pH 7.4 and 5.5. The TO-CS/Alg-NCs demonstrated enhanced cytotoxicity against two breast cancer cells, MDA-MB-231 and MCF-7, compared to the unencapsulated TO, suggesting that CS/Alg-NCs are potential nanocarriers for TO and can serve as prospective candidates for in vivo anticancer activity evaluation. [ABSTRACT FROM AUTHOR]

β-Sitosterol glucoside (SG), isolated from Senecio petasitis (Family Asteraceae), was loaded in self-nanoemulsifying drug delivery systems (SEDDS) in a trial to enhance its solubility and biological effect. Various co-surfactants were tested to prepare a successful SEDDS. The selected SG-loaded SEDDS had a droplet size of 134 ± 15.2 nm with a homogenous distribution (polydispersity index 0.296 ± 0.02). It also demonstrated a significant augmentation of SG in vitro release by 4-fold compared to the free drug suspension. The in vivo insulin sensitivity and antidiabetic effect of the prepared SG-loaded SEDDS were further assessed in streptozotocin-induced hyperglycemic rats. The hypoglycemic effect of SG-loaded nanosystem was evidenced by decreased serum glucose and insulin by 63.22% and 53.11%, respectively. Homeostasis model assessment-insulin resistance (HOMA-IR) index demonstrated a significant reduction by 5.4-fold in the diabetic group treated by SG-loaded nanosystem and exhibited reduced glucagon level by 40.85%. In addition, treatment with SG-loaded nanosystem significantly decreased serum MDA (malondialdehyde) and increased catalase levels by 38.31% and 64.45%, respectively. Histopathological investigations also supported the protective effect of SG-loaded nanosystem on the pancreas. The promising ability of SG-loaded nanosystem to ameliorate insulin resistance, protect against oxidative stress, and restore pancreatic β-cell secretory function warrants its inclusion in further studies during diabetes progression. [ABSTRACT FROM AUTHOR]

Curcumin (CUR) and D-panthenol (DPA) have been widely investigated for wound-healing treatment. In order to analyse these two compounds from a dosage form, such as polymer-based wound dressings or creams, an analytical method that allows the quantification of both drugs simultaneously should be developed. Here, we report for the first time a validated high-performance liquid chromatographic (HPLC) method coupled with UV detection to quantify CUR and DPA based on the standards set by the International Council on Harmonization (ICH) guidelines. The separation of the analytes was performed using a C18 column that utilised a mobile phase consisting of 0.001% v/v phosphoric acid and methanol using a gradient method with a run time of 15 min. The method is linear for drug concentrations within the range of 0.39–12.5 μg mL−1 (R2 = 0.9999) for CUR and 0.39–25 μg mL−1 for DPA (R2 = 1). The validated method was found to be precise and accurate. Moreover, the CUR and DPA solution was found to be stable under specific storage conditions. We, therefore, suggest that the HPLC-UV method developed in this study may be very useful in screening formulations for CUR and DPA within a preclinical setting through in vitro release studies. [ABSTRACT FROM AUTHOR]

The present work was conducted to develop a new polysaccharide‐based encapsulation system via electrostatic interactions between Prunus armeniaca gum exudates (PAGE) and Ca2+ ions to enhance the biological activity and bioavailability of curcumin. The effects of different levels of pH (6, 7, and 8) and ion concentrations (1, 3, and 5) on the particle diameter and surface charge of the samples were examined. The encapsulation efficiency in the PAGE‐based nanoparticles was realized to be 86.1%, indicating the encapsulation technique applied in this study was effective to entrap most of the curcumin within the PAGE matrix. The nanoparticles showed a smooth surface with spherical shape. Fourier transform infrared spectroscopy (FT‐IR) and X‐ray diffraction (X‐ray) studies confirmed the formation of polyelectrolyte complexation. The cumulative release of curcumin in simulated gastrointestinal tract was less than 75%, revealing a gradual release trend. Both pure curcumin and curcumin‐loaded nanoparticles were toxic to the cancer cell lines. [ABSTRACT FROM AUTHOR]

Biobased materials are expanding dramatically in various industrial applications due to their unique intrinsic properties. In this study, various chemical functionalization procedures were used to synthesize guar gum, a naturally occurring polysaccharide-based polyurea, and its iodine complexes. Firstly, guar gum was subjected to tosylation reaction using p-toluene sulphonyl chloride to introduce tosyl moieties in the polymer chain with the degree of substitution (DS) ranging between 0.16 and 1.54. Sample having the highest degree of tosyl moiety was further reacted with tris(2-aminoethyl) amine to produce 6-deoxy-6-tris(2-aminoethyl) amine derivative via nucleophilic substitution reaction to impart amino functional groups. The degree of substitution in 6-deoxy-6-tris(2-aminoethyl) amine derivative was found to be 0.59. 6-deoxy-6-tris(2-aminoethyl) amine derivative was reacted with different diisocyanates (Toluene-2,4-diisocyanate (TDI), 1,6-diisocyanatohexane (HMDI)) to produce guar gum based polyurea. Iodine complexes of the resulting polyurea were prepared by reacting with different iodinating agents. Different chemical reactions, formation of polyurea and its iodine complexes were thoroughly analyzed by different analytical techniques such as FT-IR, NMR, elemental analysis, XRD, UV–Vis spectroscopy, and a reaction scheme has been proposed. Morphological and rheological characteristics were analyzed by SEM and viscosity measurement. Thermal analysis was carried out by TGA and DSC studies. Finally, by examining the complex's UV–Vis spectra, the iodine release characteristics from polyurea‑iodine complexes were investigated. [Display omitted] [ABSTRACT FROM AUTHOR]

Cocoa butter and olive oil were used to produce cardamom essential oil (CEO) loaded nanostructured lipid carriers (NLCs). The developed NLC formulations had small size (<150 nm) and high entrapment efficiency (>90%). Scanning electron microscopy showed the round shape of NLC particles. During storage time, the particle size stayed under 150 nm, and zeta potential was almost unchanged (P > 0.05). FTIR analysis revealed no new significant chemical interaction between CEO and the NLC components. According to the in vitro release study, a large amount of CEO was encapsulated inside NLC particles (40 to 55% release in 40 days). Also, results confirmed that encapsulation of CEO by NLC was able to protect its antioxidant activity as compared to CEO emulsion (5.7 and 12.32% reduction after 30 days, respectively). CEO release from NLCs was fitted well with the Rigter–Peppas model (R2 > 93%). The results confirmed that CEO-loaded NLC could be used as a food supplement. [ABSTRACT FROM AUTHOR]

Tripartite prodrug approach is a promising strategy to improve the therapeutic efficacy of orally administrated drugs having a low bioavailability. 5-Fluorouracil is a primary chemotherapeutic agent used in the treatment of many solid tumors. The oral use of 5- fluorouracil suffers from many challenges, which are principally contributed to the erratic activity of dihydropyrimidine dehydrogenase in the GIT. In this work, five integrates were prepared as tripartite mutual prodrugs by connecting sinapic acid and four of its analogues to 5-fluorouracil through amenable ester bond. Chemical structures of the prepared integrates were defined by studying their FTIR, 1H-NMR, and 13C-NMR spectra. Initiatory cytotoxicity study was verified for these integrates via MTT test versus four cancer cell lines including HeLa, MCF-7, AMN3, and SKG. The in vitro study of releasing the active drug from the synthesized integrates was followed spectrometerically using a human serum. The results of the cytotoxicity study after 24 hr of treatment revealed that the synthesized integrates by themselves have a non-toxic activity toward the test cell lines. In contrast, the results of the same study but after 72 hr of treatment indicated the potential antitumor activity of the tested prodrugs which indicates the effective release of the active components from these prodrugs. Also, the data gathered from the release study utilizing a human serum indicated that these integrates can release the active agents pursued pseudo first order kinetics. It is concluded that the synthesized integrates could be considered as mutual prodrugs and that may be improved the clinical applications of 5-Fluorouracil. [ABSTRACT FROM AUTHOR]

A novel formulation based on nanostructured lipid carriers (NLCs) was developed to increase solubility and intestinal absorption of khellin. K-NLCs were prepared with stearic acid, hempseed oil, Brij S20, and Labrafil M 1944 CS, using the emulsification-ultrasonication method. Developed nanoparticles were chemically and physically characterized by liquid chromatography, light scattering techniques, and electron microscopy. The size, about 200 nm, was optimal for oral delivery, and the polydispersity index (around 0.26), indicated high sample homogeneity. Additionally, K-NLCs showed a spherical morphology without aggregation by microscopic analysis. The encapsulation efficiency of khellin was about 55%. In vitro release studies were carried out in media with different pH to mimic physiological conditions. K-NLCs were found to be physically stable in the simulated gastric and intestinal fluids, and they preserved about 70% of khellin after 6 h incubation. K-NLCs were also successfully lyophilized testing different lyoprotectants, and obtained freeze-dried K-NLCs demonstrated good shelf life over a month. Lastly, permeability studies on Caco-2 cells were performed to predict khellin passive diffusion across the intestinal epithelium, demonstrating that nanoparticles increased khellin permeability by more than two orders of magnitude. Accordingly, developed NLCs loaded with khellin represent a versatile formulation with good biopharmaceutical properties for oral administration, possibly enhancing khellin’s bioavailability and therapeutic effects.

Breast cancer is the most widespread malignancy in women worldwide. Nanostructured lipid carriers (NLCs) have proven effective in the treatment of cancer. NLCs loaded with imatinib (IMA) (NANIMA) were prepared and evaluated for their in vitro efficacy in MCF-7 breast cancer cells. The hot homogenization method was used for the preparation of NANIMAs. An aqueous solution of surfactants (hot) was mixed with a molten mixture of stearic acid and sesame oil (hot) under homogenization. The prepared NANIMAs were characterized and evaluated for size, polydispersity index, zeta potential, encapsulation efficiency, release studies, stability studies, and MTT assay (cytotoxicity studies). The optimized NANIMAs revealed a particle size of 104.63 ± 9.55 d.nm, PdI of 0.227 ± 0.06, and EE of 99.79 ± 0.03. All of the NANIMAs revealed slow and sustained release behavior. The surfactants used in the preparation of the NANIMAs exhibited their effects on particle size, zeta potential, encapsulation efficiency, stability studies, and release studies. The cytotoxicity studies unveiled an 8.75 times increase in cytotoxicity for the optimized NANIMAs (IC50 = 6 µM) when compared to IMA alone (IC50 = 52.5 µM) on MCF-7 breast cancer cells. In the future, NLCs containing IMA will possibly be employed to cure breast cancer. A small amount of IMA loaded into the NLCs will be better than IMA alone for the treatment of breast cancer. Moreover, patients will likely exhibit less adverse effects than in the case of IMA alone. Consequently, NANIMAs could prove to be useful for effective breast cancer treatment.

This study is focussed on micro-encapsulation of essential oils in polylactic acid (PLA) and a poly(methyl methacrylate) (PMMA) matrix as well as blends of the same. Microspheres were prepared by the solvent evaporation technique and characterised by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and Fourier transform infra-red spectroscopy (FTIR). The encapsulation efficiencies and release profiles of the essential oils were studied by gas chromatography mass spectrometry (GC-MS) and head-space solid-phase microextraction GC-MS, respectively. Furthermore, the microspheres were tested for antibacterial activity against both Gram-negative and Gram-positive bacterial strains. The results showed that the microspheres compositions (PLA/PMMA ratio) have significant effect on their characteristics. The process adopted for preparing the microspheres promoted formation of spherical particles at the sizes of 1.5–9.5 µm. The highest encapsulation efficiency of the prepared microspheres was observed in systems consisting of linalool (81.10 ± 10.0 wt. % for PLA system and 76.0 ± 3.3 wt. % for PMMA system). Confirmation was also made that the release rate of the microspheres was affected by the size of the same. [ABSTRACT FROM AUTHOR]

In the present work, a new active film based on cellulose acetate (CA) and Burdock (Arctium lappa L.) root extract (BE) was developed and the effect of different BE concentrations (0, 0.3, 0.6 and 0.9 wt%) on the mechanical, physic-chemical, thermal, antimicrobial and optical properties of CA film were investigated. Results indicated that the antimicrobial activity of CA against Aspergillus niger , Candida albicans , Staphylococcus aureus and Escherichia coli improved with increasing BE concentration. Also, there was an increase in free radical scavenger activity (DPPH), total phenol content (TPC), elongation to break (EB), contact angle (COA), color difference and water vapor transmission rate (WVTR) with BE concentration increasing. While, Young's modulus, tensile strength (TS), solubility (Sol), Water content (WC), and swelling (SW) decreased compared to control film (0 % BE). The porous and non-uniform surface in the films was observed with increasing BE concentration by a scanning electron microscope (SEM). Fourier transform infrared spectroscopic analysis (FTIR) showed that by BE adding to CA film, insignificant changes occurred compared to control film. Differential Scanning Calorimetry (DSC) results indicated that melting temperature and the glass transition temperature of CA films were decreased with BE increase. CA Film with 0.9 % BE had a 99 % weight loss after 60 days. The current research concludes that CA film containing BE can be used as an active, biodegradable and environmentally friendly edible film for food packaging. • FTIR and XRD confirmed the proper interaction of the BE with the CA film network. • The melting temperature and glass transition temperature decreased with the addition of BE, which indicated that the BE acts as a plasticizer in the film network. • BE loaded CA films could be used as edible and biodegradable films for food packaging. • SEM images indicated that the BE addition in the film changes the film's microstructure, which caused surface inhomogeneity. [ABSTRACT FROM AUTHOR]

Metamizole is an effective non-opioid analgesic drug used in the treatment of acute and chronic pain. Due to induced potentially life-threatening blood disorders, metamizole was withdrawn from market in many parts of the world, however, it is one of the most popular analgesics in Poland that is available as an over the counter drug. Patients tend to prefer capsules over tablets, as they are easier to swallow and taste better. The powder-filled capsules also have greater bioavailability and require less excipients, as compared to tablets. Polymic excipients are mainly used in capsule filling, and have influence upon the physico-chemical properties of the hard gelatin capsules and the powder formulation. The aim of the study was to determine whether various combinations of polymers impact the disintegration time and pharmaceutical availability of hard gelatin capsules with metamizole sodium. The results of our work demonstrated that the 80% of all active substance was released in all tested formulations within 15 minutes. Herein, the capsule containing lactose monohydrate had the longest release (4% after 2 min.), while capsules containing mannitol had the fastest release (81.2% after 2 min.). Moreover, the addition of HPMC to capsules with lactose brought about a slight increase in the metamizole release rate, while the addition of PVP 30 to capsules with microcrystalline cellulose slightly accelerated release. This data suggests that the use of different polymers in capsules formulation brings about changes in the physical properties of powders and modifies the release profile of metamizole. In our study, the most preferred formulation was one containing microcrystalline cellulose (good powder properties and fairly fast release).

Purpose: The aim of the present study was to formulate and optimize lipid blend-based olmesartan medoxomil (OLM) loaded nanoparticulate scaffolds (NLCs) for enhanced oral bioavailability.Method: The OLM-NLCs were formulated using dependent variables in different concentrations of solid lipid, liquid lipid, surfactant, and co-surfactant by using melt emulsification combined with ultrasonication technique. The formulations were experimentally optimized using a three-factor, three-level statistical design approach. The formulated OLM-NLCs were evaluated for various pharmaceutical quality evaluation parameters and further optimized formulation (OLM-NLCopt) was assessed for release kinetics, thermal behavior, and in vivo absorption assessment.Result: The optimized formulation (OLM-NLCopt) showed particle size (138.7 nm), PDI (0.18), and entrapment efficiency (83.65%). The comparative in vitro release study revealed OLM-NLCopt showed significantly higher (p < 0.05) drug release compare to OLM-susp. The in vivo study showed the OLM-NLCopt indicated nearly 3-fold improvement in oral bioavailability vis-a-vis OLM-susp in mice model.Conclusion: The results of the release study and pharmacokinetic study suggest the potential of OLM-NLCs for improved oral delivery. [ABSTRACT FROM AUTHOR]

Graphical abstract Abstract This work describes S-preactivated N -acetylcysteine (NAC)- and glutathione (GSH)-glycol chitosan (GC) polymer conjugates engineered as potential mucoadhesive platform. Preactivated thiomers (GC-NAC-MNA, GC-GSH-MNA) were synthesized by bond formation between GC-NAC or GC-GSH and 2-mercaptonicotinic acid (MNA) used as ligand. The presence of protected thiol moieties on this new class of thiolated GC made them not subject to oxidation. The structural modifications of the resulting derivatives were confirmed by proton Nuclear Magnetic Resonance (1H NMR) and Size Exclusion Chromatography (SEC). The conjugates displayed 91.2% and 90.1% of S-preactivation for GC-NAC-MNA and GC-GSH-MNA, respectively. The polymers were tested in ex-vivo and in vitro for their mucoadhesive properties and toxicity. The results showed that the preactivation of GC-NAC and GC-GSH increased their mucoadhesive abilities compared to their thiolated precursors by 1.4-, 4.4-fold in time of adhesion evaluated using rotating cylinder method, 1.6-, 1.5-fold in total work of adhesion (TWA) and 2.0-, 1.3-fold in maximum detachment force (MDA) determined using tensile studies, respectively. Moreover, water-uptake studies showed an improved in weight indicating water-uptake strongly dependent on derivations, before erosion occurred, whereas disintegration took place for the thiolated polymers within the first hour. The S-preactivated modification did not affect the cell viability of Caco2 cells exposed to the polymers. The release of the model drug sodium naproxen from tablets prepared with a lyophilized mixture of drug and polymer was studied via dissolution apparatus revealing that the preactivation on GC-GSH and GC-NAC involves a slowdown in the drug release rate. The results shown that the novel preactivated thiolated GC-derivatives can be considered promising excipients for the development of mucoadhesive drug delivery systems. [ABSTRACT FROM AUTHOR]

SBA-15 was functionalized by 12-tungstophosphoric acid followed by loading of poorly water soluble drug, Erythromycin and Characterized by various physicochemical techniques such as TGA, FT-IR, Nitrogen adsorption-desorption, XRD and TEM. In-vitro controlled release studies of Erythromycin in Simulated Body Fluid were carried out under stirring as well as static conditions. In order to see the influence of inorganic moiety on release rate of drug, study was also carried out with Erythromycin loaded unfunctionalized SBA-15. A study on release mechanism and release kinetics using Higuchi model, Koresmeyer-Peppas model and Extended kinetic model shows that 12-tungstophosphoric acid has significant influence on the release rate of Erythromycin. [ABSTRACT FROM AUTHOR]

ABSTRACT: Chemotherapy is one of the main treatment regimens for cancer therapy. Efficacy of chemotherapy is limited issues such as nonspecific cytotoxicity, poor aqueous solubility, and bioavailability. Targeted drug delivery is an ideal strategy to overcome these barriers. Fe3O4 magnetic nanoparticles (MNPs) as a great drug delivery system have drawn considerable attention. Functionalized nanoparticles (NPs) here were synthesized by the coprecipitation method and characterized by thermogravimetric analysis and transmission electron microscopy techniques. An anticancer agent, doxorubicin (DOX), was loaded onto the NPs and then the release behavior and cytotoxicity effects of nanodrug were determined. The pH‐sensitive behavior of drug release was observed. While the total loaded drug was released at pH 1.2 in 30 min, the amount of drug release was equal to 8% in pH 7 after 8 h. The drug‐loading efficiency was found to be 88%. Also, NPs potentiate the efficacy of the drug by increasing its cytotoxicity, in which IC50 of 57 and 39 μM for the nanodrug and drug was estimated, respectively. In conclusion, the results of the study showed that MNPs are promising vehicle for DOX delivery. [ABSTRACT FROM AUTHOR]

Drug/lense combinations have proven significant in the field of ocular therapeutics. The development of innovative systems and elaboration processes is an upcoming issue for ocular drug delivery. One challenging issue is the elaboration of drug loaded intraocular lenses (IOLs) to combine cataract surgery and post-operative treatments in a single procedure. In this work, we are studying the elaboration of such systems while using a green process using supercritical fluids for impregnating ophthalmic drugs on commercial IOLs. More particularly, rigid commercial intraocular lenses made from Poly (Methyl MethAcrylate) (PMMA), used in cataract surgery, are loaded with dexamethasone 21- phosphate disodium salt (DXP, an anti-inflammatory drug) and ciprofloxacin (CIP, an antibiotic) in order to prevent short- and mid-term postoperative complications. Supercritical impregnations were carried out in a batch mode and impregnation yields were determined through drug release kinetic studies in a solution simulating the aqueous humor. Before performing an experimental design, preliminary impregnation assays were conducted in order to delimit the operating domain. Transparent IOLs presenting an effective impregnation were obtained. The highest impregnation yields for DXP and CIP in PMMA IOLs were 18.3 and 2.8 μg drug /mg IOL respectively. Despite the low solubility of each drug in the fluid phase, homogeneous and in-depth impregnations were successfully obtained with a prolonged drug delivery (about 40 days) for most impregnation experiments. [ABSTRACT FROM AUTHOR]

Drug Delivery Systems (DDS) of known drugs are prominent candidates towards new and more-effective treatments of various infectious diseases as they may increase drug bioavailability, control drug delivery and target the site of action. In this sense, the encapsulation of Amphotericin B (AmB) in Nanostructured Lipid Carriers (NLCs) designed with pH-sensible phospholipids to target infectious tissues was proposed and suitable analytical methods were validated, as well as, proper nanoparticle characterization were conducted. Characterization assays by Dinamic Light Scattering (DLS) and Atomic Force Microscopy demonstrated spherical particles with nanometric size 268.0 ± 11.8 nm and Zeta Potential −42.5 ± 1.5 mV suggestive of important stability. DSC/TGA and FT-IR assessments suggested mechanical encapsulation of AmB. The AmB aggregation study indicated that the encapsulation provided AmB at the lowest cytotoxic form, polyaggregate. Analytical methods were developed and validated according to regulatory agencies in order to fast and assertively determine AmB in nanoparticle suspension and, in Drug Encapsulation Efficiency (EE%), release and stability studies. The quantification method for AmB in NLC suspension presented linearity in 5.05–60.60 μg mL −1 range (y = 0.07659x + 0.05344) and for AmB in receptor solution presented linearity in 0.15–10.00 μg mL −1 range (y = 54609x + 263.1), both with r ≥ 0.999. EE% was approximately 100% and according to the release results, at pH 7.4, a sustained controlled profile was observed for up 46 h. In the meantime, a micellar AmB solution demonstrated an instability pattern after 7 h of contact with the medium. Degradation and release studies under acid conditions (infectious condition) firstly depicted a prominent degradation of AmB (raw-material), with 20.3 ± 3.5% at the first hour, reaching 43.3 ± 7.0% after 7 h of study. Next, particles faster disruption in acid environment was evidenced by measuring the NLC size variation by DLS and by the loss of the bluish sheen, characteristic of the nanostructured system macroscopically observed. Finally, safety studies depicted that NLC-AmB presented reduced toxicity in fibroblast cells, corroborating with AmB aggregated form study. Therefore, an innovative AmB formulation was fully characterized and it is a new proposal for in vivo investigations. [ABSTRACT FROM AUTHOR]

In addition to offering a host of health benefits, antimicrobial (AM) wheat-based packaging is a promising form of active food packaging with great economic and environmental potential. The main objective of this study is to develop a formulation of AM wheat-based film in which the active compound, lysozyme, is incorporated into the polymeric material. A solution casting method was used in the film preparation, and lysozyme was incorporated prior to casting. The resultant film is slightly less opaque, more translucent and whitish in appearance, implying that the AM film could retain similar property with the initial opacity value of the wheat-based film. The water uptake of wheat-film is reduced with the incorporation of lysozyme. The reduction in moisture content of AM film indicates a relationship between lysozyme and water molecules in the diffusion mechanism throughout the film matrices. This film helps to reduce the growth of E. coli and B. subtilis to 1.74 and 3.48 log CFU/mL, respectively, for an incubation of 48 h. FTIR analysis implies the consistency of the chemical composition and structure of the AM film compared to the control film, which indicates that the addition of lysozyme into the wheat-based film did not affect or alter the carbonyl function groups of the wheat-based film. The study will help the researcher to discover and understand wheat-based films for incorporating antimicrobial properties and to explore new matrices for further development. [ABSTRACT FROM AUTHOR]

Breast cancer is the most common cancer diagnosed among females worldwide. Although breast cancer survival has largely improved in the past 30 years, it remains highly heterogeneous in its response to treatment. Triple-negative breast cancer (TNBC) is a subtype of breast cancer that lacks the expression of the estrogen receptor (ER), progesterone receptor (PR) and epidermal growth factor receptor-2 (Her2). While TNBC may initially be responsive to chemotherapy, recurrence and subsequent high mortality rates are frequently reported. Studies have shown curcumin and its derivatives to be effective against TNBC cell lines in vitro. To improve its anti-cancer effects, we have synthesized Fe3+⁻curcumin (Fe⁻Cur3) and Cu2+⁻curcumin (CD) complexes and investigated them experimentally. Further, CD was encapsulated into a poly(styrene)-co-maleic acid (SMA) micelle to enhance its stability. We assessed the cytotoxicity of these formulations both in vitro and in vivo. SMA⁻CD demonstrated dose-dependent cytotoxicity and abolished TNBC tumor growth in vivo. The encapsulation of the curcumin⁻copper complex improved its anti-cancer activity without overt adverse effects in a murine model of TNBC. These results provide evidence and insights into the value of nanoformulations in enhancing drug-delivery and increasing the potential therapeutic efficacy of curcumin derivatives.

The sole objective of this work was to design successful dosage oral forms of diclofenac sodium (DiNa)-loaded solid lipid microparticles (SLM) based on solidified reverse micellar solution (SRMS). Hot homogenization technique was employed to prepare DicNa SLM using a mixture goat fat and Phospholipon® 90 G as lipid matrix and Tween®-80 as mobile surfactant. Characterization based on percentage yield, morphology, particle size, zeta potential, percentage encapsulation, pH and stability of SLMs were investigated. Anti-inflammatory, gastrointestinal tract (GIT) sparing effect and pharmacokinetics were carried out in rat model after oral administration. Results showed that the SLMs were spherical and smooth. The optimized formulation (SLM-4) had particle size of 79.40 ± 0.31 µm, polydispersity index of 0.633 ± 0.190, zeta potential of −63.20 ± 0.12 mV and encapsulation efficiency of 91.2 ± 0.1% with good stability after 8 months of storage. The DicNa SLM had sustained release effect with good anti-inflammatory activity. Higher and prolonged plasma DicNa concentration was shown by the SLM-4 compared to pure drug and a conventional sample. These studies demonstrate that DicNa-loaded SLM based on SRMS could be a promising oral formulation for enhanced bioavailability, pharmacologic activity and gastrointestinal sparing effect of the NSAID, DicNa. [ABSTRACT FROM AUTHOR]

The objective of this study was to produce and characterise xylitol microcapsules for use in foods, in order to prolong the sweetness and cooling effect provided by this ingredient. Complex coacervation was employed as the microencapsulation method. A preliminary double emulsion step was performed due to the hydrophilicity of xylitol. The microcapsules obtained were characterised in terms of particle size and morphology (optical, confocal and scanning electron microscopy), solubility, sorption isotherms, FTIR, encapsulation efficiency and release study. The microcapsules of xylitol showed desirable characteristics for use in foods, such as a particle size below 109 μm, low solubility and complete encapsulation of the core by the wall material. The encapsulation efficiency ranged from 31% to 71%, being higher in treatments with higher concentrations of polymers. Release of over 70% of the microencapsulated xylitol in artificial saliva occurred within 20 min. [ABSTRACT FROM AUTHOR]

A systematic study was conducted to evaluate the crosslinker and method of incorporation for bovine serum albumin (BSA) into chitosan hybrid scaffolds (CH-ALG) for better cartilage tissue engineering applications. Formaldehyde and sodium tripolyphosphate were used crosslinkers for fabrication of CH-ALG scaffolds using BSA as growth factor by direct incorporation and microencapsulation methods. An in vitro release study of BSA with maximum release (80%) for scaffolds of formaldehyde crosslinked was found. The present findings show that the CH-ALG hybrid scaffolds have been potential use in biomedical applications. [ABSTRACT FROM AUTHOR]

A new sustained release paper-based packaging with antibacterial property was developed using the synergistic action between beta-cyclodextrin (βCD) and microfibrillated cellulose (MFC). Carvacrol, an antibacterial molecule, was included in βCD, previously grafted onto paper substrates, by impregnation. The MFC suspension was coated on the ensued substrate surface using a bar-coating process. Properties such as the Young modulus, zero-span breaking length or air permeability were characterized. Two release studies were conducted in deionized water and agar. Antibacterial tests were carried out in parallel. The mechanical properties were drastically damaged by the grafting process, whereas the barrier properties were maintained or even improved due to the MFC coating. The βCD-grafted samples allowed the gradual release of carvacrol 21 h later and with a release kinetic 24% slower in water. In agar, the association of βCD and MFC was emphasized. The samples were antibacterial for 14 h with βCD, and the addition of MFC still enhanced this period of time. A synergy between βCD and MFC was observed, paving the way for future promising development of sustained release packaging. Industrial relevance Packaging is a substantial part of our everyday life and the use of packaging materials has shown a continuous increase over time. Today, the packaging industry relies strongly on the use of petroleum-derived plastic materials, whereas it is raising both environmental and economic concerns. Besides, even in industrialized countries, food-poisoning cases still persist. As a result, the society's requirements as for the development of food-packaging materials are evolving. The use of biodegradable, bio-based food-packaging materials able to preserve and ensure the shelf-life of food is required. In response to these requirements this study proposes a new bio-based food-packaging material able to preserve better and prolong the shelf-life of food by the sustained release of antibacterial molecules. [ABSTRACT FROM AUTHOR]

The influence of excipients on the disintegration times of tablets and the release of papaverine hydrochloride (PAP) from tablets were studied. Ten different formulations of tablets with PAP were prepared by direct powder compression. Different binders, disintegrants, fillers, and lubricants were used as excipients. The release of PAP was carried out in the paddle apparatus using 0.1 N HCl as a dissolution medium. The results of the disintegration times of tablets showed that six formulations can be classified as fast dissolving tablets (FDT). FDT formulations contained Avicel PH 101, Avicel PH 102, mannitol, β-lactose, PVP K 10, gelatinized starch (CPharmGel), Prosolv Easy Tab, Prosolv SMCC 90, magnesium stearate, and the addition of disintegrants such as AcDiSol and Kollidon CL. Drug release kinetics were estimated by the zero- and first-order, Higuchi release rate, and Korsmeyer-Peppas models. Two formulations of the tablets containing PVP (K10) (10%), CPharmGel (10% and 25%), and Prosolv Easy Tab (44% and 60%) without the addition of a disintegrant were well-fitted to the kinetics models such as the Higuchi and zero-order, which are suitable for controlled- or sustained-release. [ABSTRACT FROM AUTHOR]

Pterostilbene, being extracted from many plants, has significant biological activities in preventing cancer, diabetes, and cardiovascular diseases so as to have great potential applications in pharmaceutical fields. But the poor solubility and stability of pterostilbene strictly restrained its applications. As a good protection and oral delivery system, an optimal nanoemulsion for pterostilbene was developed by using low-energy emulsification method. Systematic pseudo-ternary phase diagrams have been studied in optimization of nanoemulsion formulations. The prepared pterostilbene nanoemulsion was characterized by transmission electron microscope, Fourier transform Raman spectrum, and laser droplet size analyzer. Nanoemulsion droplets are circular with smooth margin, and the mean size is 55.8 ± 10.5 nm. The results illustrated that the nanoemulsion as oral delivery system dramatically improved the stability and solubility of pterostilbene, and in vitro release of pterostilbene was significantly improved (96.5% in pH 3.6 buffer; 13.2% in pH 7.4 buffer) in comparison to the pterostilbene suspension (lower than 21.4% in pH 3.6 buffer; 2.6% in pH 7.4 buffer). [ABSTRACT FROM AUTHOR]

The aim of present work was to prepare pulsatile drug delivery system of metoprolol succinate. In the presnt work pulsatile drug delivery system was prepared by using swellable and rupturable polymer. The polymers like Ac-di-sol and crospovideone was selected as swellable polymer while ethyl cellulose was selected as rupturable polymer. In present work, core tablet (150 mg) containing 100 mg metoprolol succinate was prepared by wet granulation technique. This prepared core tablet was coat by using 2.5% ethyl cellulose containing triethyl citrate as plasticizer. This coating solution was sprayed to core tablet to achieve different percentage of weight gain into the core tablet. The prepared film coated tablet was evaluated for in vitro drug dissolution study to get desirable immediate release of drug after lag time of 6 hour. Initially, compatibility study was carried out by differential scanning calorimetric study showing that all the excipients were compatible with the drug substance. The stability study was carried out for desired optimized batch for period of one year. The result of stability study indicates insignificant difference between before and after storage of pulsatile formulation. [ABSTRACT FROM AUTHOR]

Abstract: P-glycoprotein/MDR1 (P-gp) is a well-characterised membrane transporter relevant in drug disposition and multi-drug resistance. In this study, we aimed to investigate how far nanoparticulates impair the function of the P-gp transport system and which particle properties govern these interactions. Expression and function of P-gp was confirmed in A549 cell monolayers. Rhodamine 123 (Rh123) release studies were carried out in the presence of known inhibitors of P-gp function (i.e., cyclosporine A and verapamil), under ATP depletion (NaN3/DOG) and after acute exposure to nanoparticles (NPs) with different surface modifications, ζ-potentials and sizes (plain, carboxylated, and amine- and sulphate-modified). The cytotoxic potential of NPs on A549 monolayers was evaluated by MTT assay. The effects on P-gp protein level, after incubation with NPs, were investigated by Western blot analysis of A549 cell lysate and supernatant. Cellular retention of Rh123 was significantly (P <0.05) increased in the presence of carboxylated (100nm), amine- and sulphate-modified NPs. A slight, but not significant, decrease in Rh123 release was also observed for plain latex and carboxylated (500nm) NPs. The MTT assay demonstrated that most NPs caused only marginal levels of cytotoxicity (78–88% cell viability); the positively charged amine-NPs, however, were considerably more cytotoxic. Western blot showed that NPs did not cause any cell membrane disruption. Our findings suggest that nanomaterials can attenuate membrane transporter function depending on their size and surface properties and hence might influence the disposition of xenobiotics as well as endogenous substrates. [Copyright &y& Elsevier]

Abstract: The aim of this work was to investigate chitosomes, i.e. liposomes coated by a polyelectrolyte complex between chitosan (CH) and xantan gum (XG), as potential delivery system for oral administration of the protein C-phycocyanin. To this purpose several CH–XG-microcomplexes were prepared in aqueous lactic acid at different chitosan–xanthan gum percent ratios and rheological properties of the microcomplexes were studied to analyse the contribution of chitosan and xanthan gum in the reaction of microcomplexation. After establishing the best microcomplexes, chitosomes were prepared by coating C-phycocyanin loaded liposomes with the CH–XG hydrogels using spray-drying or freeze-drying. The chitosomes were characterized in terms of morphology, size distribution, zeta potential, swelling properties, drug release, and mucoadhesive properties. Rheological studies showed the influence of xanthan gum in the microcomplex properties. Moreover, obtained results demonstrated the effects of formulation and process variables on particle size, drug content, swelling, drug release, and especially on the mucoadhesiveness of C-PC chitosomes of CH–XG. In particular, chitosomes prepared by spray-drying technique using CH–XG in 0.5/8.0 (w/w) ratio showed a regular surface and a drug release characteristic for a Fickian diffusion of the active ingredient. The in vitro mucoadhesive study revealed that the spray-drying method is advantageous to prepare C-phycocyanin loaded chitosomes with excellent mucoadhesive properties for colonic drug delivery. [Copyright &y& Elsevier]