Chitosan-coated Liposomes Research Articles

Preparation and physicochemical characterization of N-succinyl chitosan-coated liposomes for oral delivery of grape seed extract and evaluation of its effect on pulmonary fibrosis induced by bleomycin in rats.

This study aimed to develop an oral succinyl chitosan-coated liposomal formulation containing grape seed extract and assess its therapeutic efficacy in rats with bleomycin-induced pulmonary fibrosis. N-succinyl chitosan was synthesized, and the liposomal formulations were prepared and characterized regarding phenolic content assay and morphology. Size, zeta potential, in vitro drug release, and stability. Pulmonary fibrosis was induced by intratracheal bleomycin injection, and hydroxyproline measurements, lung weight, animal body weight, as well as histopathological studies were performed. Succinyl chitosan increases the physical stability of the formulation, especially in acidic conditions. Drug release studies revealed that 66.27% of the loaded drug was released from CF2 in an acidic medium in 2 hr, but 92.31% of the drug was released in 8 hr in a pH=7 medium. An in vivo study demonstrated that rats exposed to bleomycin significantly lost weight, while those treated with CF2 (400 mg/kg) partially regained weight. Bleomycin treatment increased the mean lung weight and the amount of hydroxyproline in the lungs; these values were significantly decreased in the group treated with 400 mg/kg CF2 (P<0.05). Histopathological examination confirmed that treatment with 400 mg/kg CF2 improved lung fibrosis. In rats, oral administration of N-succinyl chitosan-coated liposomes containing grape seed extract at the 400 mg/kg dose ameliorates bleomycin-induced pulmonary fibrosis.

Optimization of Nasal Liposome Formulation of Venlafaxine Hydrochloride using a Box-Behnken Experimental Design

Intranasal administration is among the most effective alternatives to deliver drugs directly to the brain and prevent first-pass metabolism. Venlafaxine-loaded liposomes are biocompatible carriers that enhance transport qualities over the nasal mucosa. This research aimed to develop, formulate, characterize, and observe the prepared formulation. The formulation was developed using the thin-film hydration technique. The response surface plot interrelationship between three independent variables are lipid, cholesterol and polymer and four dependent variables such as particle size, percentage entrapment efficiency, and percentage drug release were ascertained using the Box-Behnken design. The drug-release chitosan-coated liposomes were reported to have a particle size distribution, entanglement efficiency, and 84%, respectively, of 191 ± 34.71 nm, 94 ± 2.71% and 94 ± 2.71%. According to in vitro investigations, liposomes as a delivery system for the nasal route provided a more sustained drug release than the oral dosing form. The intranasal administration of venlafaxine liposomal vesicles effectively enhanced the absolute bioavailability, retention time, and brain delivery of venlafaxine.

Hepatocyte-targeted delivery using oleanolic acid-loaded liposomes for enhanced hepatocellular carcinoma therapy.

Drug-loaded liposomes have been shown to be effective in the treatment of hepatocellular carcinoma (HCC). However, the systemic non-specific distribution of drug-loaded liposomes in tumor patients is a critical therapeutic challenge. To address this issue, we developed galactosylated chitosan-modified liposomes (GC@Lipo) that could selectively bind to the asialoglycoprotein receptor (ASGPR), which is highly expressed on the membrane surface of HCC cells. Our study demonstrated that the GC@Lipo significantly enhanced the anti-tumor efficacy of oleanolic acid (OA) by enabling targeted drug delivery to hepatocytes. Remarkably, treatment with OA-loaded GC@Lipo inhibited the migration and proliferation of mouse Hepa1-6 cells by upregulating E-cadherin expression and downregulating N-cadherin, vimentin, and AXL expressions, compared to a free OA solution and OA-loaded liposomes. Furthermore, using an axillary tumor xenograft mouse model, we observed that OA-loaded GC@Lipo led to a significant reduction in tumor progression, accompanied by concentrated enrichment in hepatocytes. These findings strongly support the clinical translation of ASGPR-targeted liposomes for the treatment of HCC.

Cationic biopolymer decorated Asiatic Acid and Centella asiatica extract incorporated liposomes for treating early-stage Alzheimer's disease: An In-vitro and In-vivo investigation.

Background:Asiatic acid (AA) is a naturally occurring triterpenoid derivative of Centella asiatica (CA) with neuroprotective effect.The study aimed to design an ideal oral drug delivery system to treat Alzheimer's disease (AD) and develop chitosan-embedded liposomes comprising an extract of CA (CLCAE) and compare them with the chitosan-coated liposomes of asiatic acid (CLAA) for oral delivery to treat the initial phases of AD. Methods:The solvent evaporation technique was used to develop CLCAE and CLAA, optimised with the experiment's design, and was further evaluated. Results:Nuclear magnetic resonance (NMR) studies confirmed coating with chitosan. Transmission electron microscopy(TEM) and atomic force microscopy (AFM) indicated the successful formation of CLCAE and CLAA. Differential scanning colorimetry (DSC) confirmed the drug-phospholipid complex. Furthermore, the rate of in vitrorelease of CLCAE and CLAA was found to be 69.43±0.3 % and 85.3±0.3 %, respectively, in 24 h. Ex vivopermeation of CLCAE and CLAA was found to be 48±0.3 % and 78±0.3 %, respectively. In the Alcl3-induced AD model in rats, disease progression was confirmed by Y-maze, the preliminary histopathology evaluation showed significantly higher efficacy of the prepared liposomes (CLCAE and CLAA) compared to the Centella asiatica extract (CAE) and they were found to have equivalent efficacy to the standard drug (rivastigmine tartrate). The considerable increase in pharmacodynamic parameters in terms of neuronal count in the CLAA group indicated the protective role against Alcl3 toxicity and was also confirmed by assessing acetylcholine (Ach) levels. The pharmacokinetic study, such as C max, T max, and area under curve (AUC) parameters, proved an increase in AA bioavailability in the form of CLAA compared to the pure AA and CLCAE forms. Conclusion:The preclinical study suggested that CLAA was found to have better stability and an ideal oral drug delivery system to treat AD.

Effect of Chitosan Coating for Efficient Encapsulation and Improved Stability under Loading Preparation and Storage Conditions of Bacillus Lipopeptides

This study aims to evaluate the effect of chitosan coating on the formation and properties of Bacillus cyclic lipopeptide (CLP)-loaded liposomes. A nanoencapsulation strategy for a chitosan-coated liposomal system using lecithin phospholipids for the entrapment of antibiotic CLP prepared from Bacillus subtilis KB21 was developed. The produced chitosan-coated CLP liposome had mean size in the range of 118.47-121.67 nm. Transmission electron microscopy showed the spherical-shaped vesicles. Fourier transform infrared spectroscopy findings indicated the successful coating of the produced CLP-loaded liposomes by the used chitosan. Liposomes coated with 0.2% and 0.5% chitosan concentration decreased the surface tension by 7.3-12.1%, respectively, and increased the CLP content by 15.1-27.0%, respectively, compared to the uncoating liposomes. The coated concentration of chitosan influenced their CLP loading encapsulation efficiency and release kinetics. The physicochemical results of the dynamic light scattering, CLP capture efficiency and long-term storage capacity of nanocapsules increased with chitosan coating concentration. Furthermore, the chitosan-coated liposomes exhibited a significant enhancement in the stability of CLP loading liposomes. These results may suggest the potential application of chitosan-coated liposomes as a carrier of antibiotics in the development of the functional platform.

Quaternized chitosan-coated liposomes enhance immune responses by co-delivery of antigens and resveratrol

Co-localization of antigens and immunomodulators in the same antigen-presenting cells (APCs) can powerfully activate APCs and enhance immune responses. In this study, the immunomodulator resveratrol (Res) was encapsulated into quaternized chitosan (QCS) - coated liposomes for developing a new nanoparticle delivery system (QCS-Res-LP), and ovalbumin (OVA) was selected as a model antigen and adsorbed on the surface of QCS-Res-LP. The results showed that the particle size of QCS-Res-LP was 96.3 ± 3.52 nm; the PDI value was 0.280 ± 0.010; the Zeta potential was 9.59 ± 0.36 mV. QCS-Res-LP could encapsulate 76.22 ± 1.02 % resveratrol and adsorb 88.2 ± 16.3 % antigen. QCS-Res-LP effectively promoted the co-uptake of antigen and Res by dendritic cells (DCs) with 50-fold greater than resveratrol liposomes (Res-LP). QCS-Res-LP promoted expression levels of CD80, CD86, IL-2, and IL-12 in DCs. QCS-Res-LP did not cause hemolysis. The levels of ovalbumin-specific IgG antibodies and cytokines were significantly increased in mice vaccinated with ovalbumin-absorbed QCS-Res-LP, which induced a mixed Th1/Th2 immune response. In conclusion, these results demonstrated that QCS-coated liposomes enable the co-delivery of antigens and immunomodulators to induce strong and durable immune responses.

Novel Metoprolol-Loaded Chitosan-Coated Deformable Liposomes in Thermosensitive In Situ Gels for the Management of Glaucoma: A Repurposing Approach.

Glaucoma is a long-term eye disease associated with high intraocular pressure (IOP), which seriously damages the eyes, causing blindness. For successful therapy, potent drugs and delivery systems are required. Metoprolol (MT) is believed to help reduce elevated IOP. The paradigm of ocular therapeutics may be changed by the integration of chitosan-coated liposomes (CLPs) with thermosensitive in situ gel (ISG). Therefore, MT-CLPs were developed and characterized and compared to uncoated ones (MT-LPs). Furthermore, MT-LP- and MT-CLP-loaded ISGs were prepared and characterized in in vitro, ex vivo, and in vivo studies. MT-LPs and MT-CLPs displayed spherical shapes with nanosize range, reasonable EE%, and significant bioadhesion. The zeta potential changed from negative to positive after CS coating. The extended in vitro drug release of MT-CLPs showed significant mucin mucoadhesion. The formed ISGs were homogeneous with a pH range of 7.34 to 7.08 and a rapid sol–gel transition at physiological temperature. MT-ISG1 (MT-LP) and MT-ISG2 (MT-CLPs-0.5) could increase ocular permeability by 2-fold and 4.4-fold compared to MT-ISG (pure MT). MT-ISG2 demonstrated significantly reduced IOP in rabbits without causing any irritation. In conclusion, MT-ISG2 markedly enhanced corneal permeability and reduced IOP. They would be promising carriers for MT for glaucoma management.

Chitosan-based delivery system enhances antimicrobial activity of chlorhexidine.

Infected chronic skin wounds and other skin infections are increasingly putting pressure on the health care providers and patients. The pressure is especially concerning due to the rise of antimicrobial resistance and biofilm-producing bacteria that further impair treatment success. Therefore, innovative strategies for wound healing and bacterial eradication are urgently needed; utilization of materials with inherent biological properties could offer a potential solution. Chitosan is one of the most frequently used polymers in delivery systems. This bioactive polymer is often regarded as an attractive constituent in delivery systems due to its inherent antimicrobial, anti-inflammatory, anti-oxidative, and wound healing properties. However, lipid-based vesicles and liposomes are generally considered more suitable as delivery systems for skin due to their ability to interact with the skin structure and provide prolonged release, protect the antimicrobial compound, and allow high local concentrations at the infected site. To take advantage of the beneficial attributes of the lipid-based vesicles and chitosan, these components can be combined into chitosan-containing liposomes or chitosomes and chitosan-coated liposomes. These systems have previously been investigated for use in wound therapy; however, their potential in infected wounds is not fully investigated. In this study, we aimed to investigate whether both the chitosan-containing and chitosan-coated liposomes tailored for infected wounds could improve the antimicrobial activity of the membrane-active antimicrobial chlorhexidine, while assuring both the anti-inflammatory activity and cell compatibility. Chlorhexidine was incorporated into three different vesicles, namely plain (chitosan-free), chitosan-containing and chitosan-coated liposomes that were optimized for skin wounds. Their release profile, antimicrobial activities, anti-inflammatory properties, and cell compatibility were assessed in vitro. The vesicles comprising chitosan demonstrated slower release rate of chlorhexidine and high cell compatibility. Additionally, the inflammatory responses in murine macrophages treated with these vesicles were reduced by about 60% compared to non-treated cells. Finally, liposomes containing both chitosan and chlorhexidine demonstrated the strongest antibacterial effect against Staphylococcus aureus. Both chitosan-containing and chitosan-coated liposomes comprising chlorhexidine could serve as excellent platforms for the delivery of membrane-active antimicrobials to infected wounds as confirmed by improved antimicrobial performance of chlorhexidine.

Improving the stability and bioactivity of curcumin using chitosan-coated liposomes through a combination mode of high-pressure processing

This study used chitosan-coated liposomes of curcumin (cur-chitosomes) coupled with a combination mode of high-pressure processing (HPP) and ethanol injection to improve the bioactivity, preservation, and thermal stability of curcumin. The results revealed cur-chitosomes presented the best thermal stability and encapsulation efficiency. With 0.1% chitosan addition, the encapsulation efficiency increased from 73.8 to 84.0%, accompanying with less increases on particle size and polydispersity index. Storage stability for 28 days incubation demonstrated the particle size of cur-chitosomes remained at a constant value, which presented the long thermal stability due to the static electrostatic repulsive force. The stability of cur-chitosomes presented high value of 85.3% at degradation conditions of 25 °C and 480 min. With thermal kinetic calculation, the half-life of curcumin-loaded liposomes and cur-chitosomes were 625 and 1250 min at 25 °C, so liposome formation and chitosan addition in curcumin could increase the storage time. Over 104 CFU/g Escherichia coli, Staphylococcus aureus, and Staphylococcus aureus could be completely sterilized in the preparation of cur-chitosomes at 400 MPa HPP. Consequently, chitosomes by HPP not only prevented the thermal degradation of heat-sensitive substances but also enhanced the storage stability and the sterilization effect in a non-thermal process.

Chitosan-Coated Liposomes: The Strategy to Reduce Intestinal Toxicity and Improve Bioavailability of Oral Vinorelbine.

In recent years, the oral administration of vinorelbine has gradually replaced intravenous administration in the treatment of several types of tumors. Even though the risk of phlebitis is avoided with oral administration, oral vinorelbine is still not a highly patient-compliant route due to the severe gastrointestinal toxicity. Vinorelbine-loaded liposomes with high encapsulation efficiency and suitable particle size were prepared using the ammonium sulfate gradient method. Chitosan-coated liposomes showed the slowest in vitro release compared to uncoated liposomes and vinorelbine solution. No damage was observed in the intestinal epithelial cells of mice orally administered with coated vinorelbine liposomes due to the low presence of the free drug in the gastrointestinal tract and the LD50 was increased from 129.83 to 182.25mg/kg compared to oral vinorelbine solution. In addition, the positive surface potential of chitosan-coating endowed liposomes with mucosal adhesive function, delaying the time to reach the peak plasma concentration of vinorelbine from 1 to 4h after administration. And bioavailability was increased to 2.1-fold compared to vinorelbine solution. In short, a new strategy to address the severe gastrointestinal side effects of oral vinorelbine has been developed.

Encapsulation efficiency and oral delivery stability of chitosan–liposome‐encapsulated immunoglobulin Y

The degradation of acidic gastric juice on immunoglobulin Y (IgY) leads to destruction on the structural and loss of the bioactivity, limiting the bioavailability of oral IgY and its research or application in adjuvant treatment of diseases. In this work, it was surmounted with IgY-loaded chitosan-liposomes prepared by supercritical carbon dioxide-assisted method. A range of chitosan concentrations (0%, 0.5%, 0.8%, 1.1%, and 1.4%) were selected to explore the influence of chitosan concentration on the encapsulation effectiveness, stability, and in vitro-simulated digestive release properties of liposome-encapsulated IgY. The results displayed that owing to the robust interaction between chitosan and liposomes, the particle size, encapsulation efficiency, and stability of liposomes reached the optimal state at a chitosan concentration of 0.8%, with the encapsulation efficiency reaching 77.51%. Moreover, the liposomes could be stored at 4°C for 9 days without obvious sedimentation. The zeta potential of liposomes containing 0.8% chitosan was higher than that of samples without chitosan at high salt concentration treatment. In vitro release experiments demonstrated that liposomes fitted well in the Peppas equation. Chitosan-coated liposomes were capable of delaying the release of IgY in the stomach during simulated digestion, allowing more IgY to be released in the intestine. To sum up, Chitosan played a vital role in maintaining the stability and encapsulation of IgY, and the results of this work provide a theoretical basis for the development and utilization of chitosan and the protection of activity of IgY when administered orally. PRACTICAL APPLICATION: IgY serves as a bioactive substance with anti-inflammatory, antibacterial, and antioxidant functions. However, it is far from satisfactory for the oral delivery activity of IgY. Encapsulation of liposomes contributed to alleviate the release of IgY in the stomach. However, liposomes were less stable and not efficient enough to encapsulate IgY. This study demonstrated that the addition of 0.8% chitosan could effectively enhance the encapsulation efficiency of liposomes and improved the stability of liposomes. It might contribute to the solution of the oral delivery activity of IgY and provide a promising idea for the utilization of chitosan.

Potential Use of Tailored Citicoline Chitosan-Coated Liposomes for Effective Wound Healing in Diabetic Rat Model.

PurposeThis study aimed to formulate citicoline-loaded chitosan-coated liposomes (CT-CS-LPs) for topical administration and evaluated for wound healing in a diabetic animal model.MethodsCT-LPs were formulated via a thin-film hydration approach and coated with chitosan (CS). Box-Behnken statistical design investigated the effects of lipid amount, chitosan concentration, and cholesterol amount on vesicle diameter, surface charge, and entrapment efficiency. The potential of the optimized CT-CS-LPs gel for wound healing was further evaluated in streptozocin-induced diabetic rats. The different healing stages were evaluated by several techniques, including general and special staining techniques, in addition to antibody immunohistochemistry.ResultsThe optimized CT-CS-LPs obtained had a mean size of 211.6 nm, a 50.7% entrapment efficiency, and a positive surface charge of 32.1 mV. In addition, the optimized CT-CS-LPs exhibited in vitro sustained release behavior. The in vivo experiments revealed that treatment with the optimized CT-CS-LPs boosts the healing process of the skin wound in diabetic rats by reducing inflammation, accelerating re-epithelization, angiogenesis, fibroblast proliferation, and connective tissue remodeling, leading to rapid wound closure.ConclusionChitosan-coated liposomes containing citicoline have emerged as a potential approach for promoting the healing process in diabetic rats. However, the therapeutic effectiveness of the suggested approach in diabetic patients needs to be investigated.

Pharmacokinetics study of chitosan-coated liposomes containing sumatriptan in the treatment of migraine.

Background:Sumatriptan is a routine medication in the treatment of migraine and cluster headache that is generally given by oral or parental routes. However, a substantial proportion of patients suffer severe side effects. The aim of this study was to investigate the physicochemical characterization and pharmacokinetic parameters of a novel delivery system for sumatriptan succinate (SS) using nanoliposomes (NLs) coated by chitosan (CCLs) to optimize the formulations to enhance its bioavailability.Methods:The new formulation was used to minimize drug particle size and extend its release and bioavailability. The mean particle size and entrapment efficiency for NLs and CCls were optimized and the formulations with better characteristics were chosen for in vivo studies. The concentration-time profile of intravenous SS, intranasal SS, SS-NLs, and CCLs were examined in a rabbit model.Results:The results demonstrated that CCLs were absorbed more rapidly from nasal drops containing chitosan compared to those of SS and SS-NLs as indicated by a shorter tmax, and a higher Cmax in both states. A comparison of the AUC (0-240 min) values revealed that chitosan improved the extent of SS absorption for CCLs formulation. The results of the present study indicated that loading SS into the liposome and coating with chitosan improves drug absorption and a large amount of the drug can be efficiently delivered into the systemic circulation.Conclusion:The liposomal and chitosan formulations of SS had better kinetic behavior than the soluble form in the animal model.

Eugenol encapsulation into conventional liposomes and chitosan-coated liposomes: A comparative study

The aim of this study is to investigate the effect of chitosan coating layer and molecular weight on the characteristics of liposomes encapsulating eugenol, a volatile essential oil component. Two approaches were used: eugenol-loaded conventional liposomes were prepared and then coated with chitosan (referred to as chitosan-coated liposomes or chitosomes), blank empty chitosomes were prepared and then eugenol was added to join the structures (referred to as preformed chitosomes). Eugenol-loaded liposomes and -chitosomes were characterized and compared in terms of size, eugenol encapsulation efficiency (EE), eugenol loading rate (LR), and phospholipid and cholesterol incorporation rates (IR). Compared to conventional liposomes, the presence of chitosan coating layer increased significantly the mean particle size in a concentration dependent manner. Increasing the chitosan molecular weight led to an increase in cholesterol incorporation in liposomes. High EE of eugenol was obtained in all formulations (above 68.8%). However, both phospholipid and eugenol incorporation rates decreased in chitosomes. All chitosomal formulations enhanced the antioxidant activity of eugenol compared to the uncoated ones and maintained the eugenol encapsulation after 2 months of storage at 4 °C. The retention efficiency (RE) of eugenol into preformed blank conventional liposomes and chitosomes was assessed using the dialysis technique. After 21 days, the RE of eugenol reached 41, 45.5 and 80%, respectively in preformed liposomes and preformed chitosomes with low and high molecular weight. The results have demonstrated the incorporation of eugenol into both preformed systems, with the ability of chitosan to enhance its incorporation, especially with the highest molecular weight.

Characterization and Caco-2 Cell Transport Assay of Chito-Oligosaccharides Nano-Liposomes Based on Layer-by-Layer Coated.

Chito-oligosaccharides (COSs) were encapsulated by the film-ultrasonic method into three nano-liposomes, which were uncoated liposomes (COSs-Lip), chitosan-coated liposomes (CH-COSs-Lip), and sodium alginate (SA)/chitosan (CH)-coated liposomes (SA/CH-COSs-Lip). The physicochemical and structural properties, as well as the stability and digestive characteristics, of all three nano-liposomes were assessed in the current study. Thereafter, the characteristics of intestinal absorption and transport of nano-liposomes were investigated by the Caco-2 cell monolayer. All nano-liposomes showed a smaller-sized distribution with a higher encapsulation efficiency. The ζ-potential, Z-average diameter (Dz), and polydispersity index (PDI) demonstrated that the stability of the SA/CH-COSs-Lip had much better stability than COSs-Lip and CH-COSs-Lip. In addition, the transport of the nano-liposomes via the Caco-2 cell monolayer indicated a higher transmembrane transport capacity. In summary, the chitosan and sodium alginate could serve as potential delivery systems for COSs to fortify functional foods and medicines.

Cross-linked chitosan-coated liposomes for encapsulation of fish-derived peptide

The aim of this work was to develop novel hybrid nanocarriers made of liposomes coated with chitosan (CS) cross-linked with sodium tripolyphosphate (TPP), named CS-TPP/liposomes, for fish-purified antioxidant peptide fractionated by RP-HPLC (F5). The produced nanodispersion (peptide-loaded CS-TPP/liposomes) was characterized by dynamic light scattering (DLS), high-resolution transmission electron microscopy (HRTEM), Fourier transform infrared (FT-IR) spectroscopy, and differential scanning calorimetry (DSC). The mean nanoparticle sizes of these uncoated and CS-TPP coated liposomes were found to be 409.2 and 687.4 nm, respectively, and the obtained polydispersity index (PDI) was ≤0.2. HRTEM revealed the spherical shape and smooth surface of the produced peptide-loaded nanovesicles. FT-IR spectroscopy revealed that the liposomes have been successfully coated by CS-TPP. In addition, DSC findings indicated enhanced electrostatic interactions among CS and lecithin molecules, leading to an increase in the melting (Tm) and decomposition temperature (Td) in peptide-loaded CS-TPP/liposomes hybrid system. Furthermore, the antioxidant activity of the loaded fish-purified antioxidant peptide to CS-TPP/liposomes was retained as confirmed by the employed free radical scavenging assay. The proposed hybrid system represents a promising idea for the delivery of protein hydrolysate and peptide fractions thereof in nutraceutical and functional foods applications.

Formulation of Piperine-Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation.

The present research work is designed to prepare and evaluate piperine liposomes and piperine–chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (−7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly (p < 0.001)) reduced the IC50 when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.

A study on chitosan-coated liposomes as a carrier of bovine serum albumin as oral protein drug

The development of protein drug liposomes was limited due to the instability of the structure of liposomes, such as easy aggregation, easy fusion, and drug leakage. The object of this work was to prepare bovine serum albumin (BSA) loaded liposomes (BSA-Lip) using BSA as a protein model drug and then BSA-Lip was further coated with chitosan (CH-BSA-Lip) in order to improve the stability of phospholipid bilayer membrane. It was found that the particle size of BSA-Lip increased after being coated with chitosan and the surface potential changed from negative charge to positive charge due to the electrostatic interaction between liposomes and chitosan. After chitosan coating, the encapsulation efficiency of liposomes also increased due to the interaction between positively charged chitosan and negatively charged BSA. Fourier transform infrared spectroscopy analysis confirmed that BSA was encapsulated into liposomes and chitosan was successfully coated on the surface of liposomes. Transmission electron microscopy showed that the particles were nanosized and spherical. The physical stability and in vitro digestion stability of liposomes were examined by observing the changes of particle size and potential. It was found that chitosan coating enhanced the stability of liposomes significantly. The in vitro release profile of CH-BSA-Lip possessed a slow release behavior, and BSA release was governed by both diffusion and dissolution from phospholipid bilayer.

Evaluation of Antinociceptive Effects of Chitosan-Coated Liposomes Entrapping the Selective Kappa Opioid Receptor Agonist U50,488 in Mice.

Background and Objectives: The selective kappa opioid receptor agonist U50,488 was reported to have analgesic, cough suppressant, diuretic and other beneficial properties. The aim of our study was to analyze the effects of some original chitosan-coated liposomes entrapping U50,488 in somatic and visceral nociceptive sensitivity in mice. Materials and Methods: The influence on the somatic pain was assessed using a tail flick test by counting the tail reactivity to thermal noxious stimulation. The nociceptive visceral estimation was performed using the writhing test in order to evaluate the behavioral manifestations occurring as a reaction to the chemical noxious peritoneal irritation with 0.6% acetic acid (10 mL/kbw). The animals were treated orally, at the same time, with a single dose of: distilled water 0.1 mL/10 gbw; 50 mg/kbw U50,488; 50 mg/kbw U50,488 entrapped in chitosan-coated liposomes, according to the group they were randomly assigned. Results: The use of chitosan-coated liposomesas carriers for U50,488 induced antinociceptive effects that began to manifest after 2 h, andwere prolonged but with a lower intensity than those caused by the free selective kappa opioid in both tests. Conclusion: In this experimental model, the oral administration of nanovesicles containing the selective kappa opioid agonist U50,488 determined a prolonged analgesic outcome in the tail flick test, as well as in the writhing test.

Preparation, characterization and release behavior of chitosan-coated nanoliposomes (chitosomes) containing olive leaf extract optimized by response surface methodology

The online version contains supplementary material available at (10.1007/s13197-021-04972-2).