Chitosan-coated Liposomes Research Articles

Chitosomes incorporated with sweet basil oil (Ocimum basilicum L.): Protecting anthracnose and preserving the postharvest quality of 'Nam Dok Mai' mangoes

Mango cv. 'Nam Dok Mai' is highly susceptible to anthracnose and undergoes rapid degeneration once it reaches ripeness. The objective was to compare the effectiveness of sweet basil oil, liposome-incorporated with sweet basil oil and chitosan-coated liposomes (Chitosomes) incorporated with sweet basil oil treatments in suppressing Colletotrichum gloeosporioides growth, both in vitro and in vivo. The particle size, zeta potential, total phenol content and antioxidant activity of sweet basil oil and liposomes- and chitosomes-containing sweet basil oil were comparable. Furthermore, the study examined the effectiveness of chitosomes incorporated with sweet basil oil in preserving the postharvest quality of mangoes during storage at 25±2ºC. The result demonstrated that sweet basil oil could slow down the growth of Colletotrichum gloeosporioides mycelium. Chitosomes containing 4 and 6 µL mL−1 of sweet basil oil effectively slowed down the mycelium growth and disease incidence in inoculated mangoes compared to liposomes containing sweet basil oil. Chitosomes containing 4 µL mL−1 of sweet basil oil was chosen to investigate its effectiveness in preserving the postharvest quality of the mangoes compared to treatments using solely sweet basil oil and liposomes-containing sweet basil oil. Compared to other treatments, the treatment effectively inhibited disease incidence, delayed weight loss, and enhanced antioxidant activity in the mangoes. Both liposomes- and chitosomes- containing sweet basil oil maintained firmness, induced antioxidant enzyme activities, and delayed the ripening of the mangoes. To summarise, the chitosomes treatment is an effective approach to preserving the postharvest quality of the mangoes during storage.

Preparation and characterization of moringin-loaded chitosan-coated liposomes and their antibacterial activity against Staphylococcus aureus

This study aimed to improve the stability of moringin and clarify the inhibitory mechanisms of moringin-loaded chitosan-coated liposomes (MR-CS-LPs) against Staphylococcus aureus. Optimisation of MR-CS-LPs was conducted using the response surface methodology, and extensive characterization was performed. The anti-bacterial activity of MR-CS-LPs was assessed by determining the minimum inhibitory concentration (MIC) and conducting growth curve analyses. The effects of MR-CS-LPs on S. aureus cell wall and membrane integrity were investigated using techniques such as scanning electron microscopy and physical and chemical analyses. Apoptotic effects were evaluated by examining oxidative stress parameters, and the impact on S. aureus biofilm formation was explored. An LC–MS/MS analysis provided insights into the inhibitory mechanism of MR-CS-LPs against S. aureus. The results indicated that MR-CS-LPs achieved an encapsulation rate of 69.02 %. Furthermore, they demonstrated potent anti-bacterial activity against S. aureus, with an MIC of 0.125 mg/mL. MR-CS-LPs disrupted cell wall and membrane integrity, resulting in macromolecule leakage, induced oxidative stress–mediated apoptosis and effectively suppressed biofilm formation, ultimately leading to bacterial death. Metabolomics analysis revealed that MR-CS-LPs inhibit S. aureus by regulating pyruvate pathways. These findings affirm that MR-CS-LPs possess significant anti-microbial properties, underscoring their potential as effective anti-microbial agents against S. aureus.

Chitosan-Coated Liposome Formulations for Encapsulation of Ciprofloxacin and Etoposide.

Cancer and bacterial infections rank among the most significant global health threats. accounting for roughly 25 million fatalities each year. This statistic underscores the urgent necessity for developing novel drugs, enhancing current treatments, and implementing systems that boost their bioavailability to achieve superior therapeutic outcomes. Liposomes have been recognised as effective carriers; nonetheless, they encounter issues with long-term stability and structural integrity, which limit their pharmaceutical applicability. Chitosomes (chitosan-coated liposomes) are generally a good alternative to solve these issues. This research aims to demonstrate the effective individual encapsulation of ciprofloxacin (antibacterial, hydrophilic) and etoposide (anticancer, hydrophobic), within chitosomes to create more effective drug delivery systems (oral administration for ciprofloxacin, parenteral administration for etoposide). Thus, liposomes and chitosomes were prepared using the thin-film hydration technique and were characterised through ATR-FTIR, Dynamic Light Scattering (DLS), zeta potential, and release profiling. In both cases, the application of chitosomes enhanced long-term stability in size and surface charge. Chitosome-encapsulated ciprofloxacin formulations exhibited a slower and sustained release profile, while the combined effect of etoposide and chitosan showed heightened efficacy against the glioblastoma cell line U373. Therefore, coating liposomes with chitosan improved the encapsulation system's properties, resulting in a promising method for drug delivery.

Comparative In Vitro Study between Biocompatible Chitosan-Based Magnetic Nanocapsules and Liposome Formulations with Potential Application in Anti-Inflammatory Therapy.

This study describes the comparison between the interaction of a series of peptide-functionalized chitosan-based nanocapsules and liposomes with two cell lines, i.e., mouse macrophages RAW 264.7 and human endothelial cells EA.hy926. Both types of nanocarriers are loaded with magnetic nanoparticles and designed for anti-inflammatory therapy. The choice of these magnetic nanostructures is argued based on their advantages in terms of size, morphology, chemical composition, and the multiple possibilities of modifying their surface. Moreover, active targeting might be ensured by using an external magnetic field. To explore the impact of chitosan-based nanocapsules and liposomes on cell cytophysiology, the cell viability, using the MTT assay, and cell morphology were investigated. The results revealed low to moderate cytotoxicity of free nanocapsules and significant cytotoxicity induced by chitosan-coated liposomes loaded with dexamethasone, confirming its release from the delivery system. Thus, after 48 h of treatment with nanocapsules, the viability of RAW 264.7 cells varied between 88.18% (OCNPM-1I, 3.125 µg/mL) and 76.37% (OCNPM-1, 25 µg/mL). In the same conditions, EA.hy926 cell viability was between 99.91% (OCNPM-3, 3.125 µg/mL) and 75.15% (OCNPM-3, 25 µg/mL) at the highest dose (25 µg/mL), the values being comparable for both cell lines. Referring to the cell reactivity after dexamethasone-loaded liposome application, the lowest viability of RAW 264.7 cells was 41.25% (CLDM5CP-1, 25 µg/mL) and 58.20% (CLDMM2CP-1 1.25 µg/mL) in the endothelial cell line, proving a selective character of action of nanocarriers. The cell morphology test, performed to support and confirm the results obtained by the MTT test, revealed a differentiated response for the two types of nano-carriers. As expected, an intense cytotoxic effect in the case of dexamethasone-loaded liposomes and a lack of cytotoxicity for drug-free nanocapsules were noticed. Therefore, our study demonstrated the biocompatible feature of the studied nanocarriers, which highlights them for future research as potential drug delivery systems for pharmacological applications, including anti-inflammatory therapy.

Ceftazidime and Usnic Acid Encapsulated in Chitosan-Coated Liposomes for Oral Administration against Colorectal Cancer-Inducing Escherichia coli.

Escherichia coli has been associated with the induction of colorectal cancer (CRC). Thus, combined therapy incorporating usnic acid (UA) and antibiotics such as ceftazidime (CAZ), co-encapsulated in liposomes, could be an alternative. Coating the liposomes with chitosan (Chi) could facilitate the oral administration of this nanocarrier. Liposomes were prepared using the lipid film hydration method, followed by sonication and chitosan coating via the drip technique. Characterization included particle size, polydispersity index, zeta potential, pH, encapsulation efficiency, and physicochemical analyses. The minimum inhibitory concentration and minimum bactericidal concentration were determined against E. coli ATCC 25922, NCTC 13846, and H10407 using the microdilution method. Antibiofilm assays were conducted using the crystal violet method. The liposomes exhibited sizes ranging from 116.5 ± 5.3 to 240.3 ± 3.5 nm and zeta potentials between +16.4 ± 0.6 and +28 ± 0.8 mV. The encapsulation efficiencies were 51.5 ± 0.2% for CAZ and 99.94 ± 0.1% for UA. Lipo-CAZ-Chi and Lipo-UA-Chi exhibited antibacterial activity, inhibited biofilm formation, and preformed biofilms of E. coli. The Lipo-CAZ-UA-Chi and Lipo-CAZ-Chi + Lipo-UA-Chi formulations showed enhanced activities, potentially due to co-encapsulation or combination effects. These findings suggest potential for in vivo oral administration in future antibacterial and antibiofilm therapies against CRC-inducing bacteria.

Functional mango juice with apigenin encapsulated in spray-dried chitosan-coated liposomes: Characterisation, in-vitro gastrointestinal release, sensory acceptance, and storage stability

Given the diverse health benefits of apigenin (AP), functional foods containing AP might interest the health-conscious market. However, the poor aqueous solubility of AP hinders its direct incorporation into food products. To overcome these limitations, AP was encapsulated in spray-dried unilamellar liposomes coated with chitosan. This study investigated the potential of spray-dried chitosan-coated AP liposomes (SCAL) for delivering AP in mango juice. The incorporation of SCAL did not alter the juice's proximate compositions or substantially affect its physicochemical properties. Mango juice with SCAL attained a comparable sensory acceptance to the control juice, with the added benefit of higher antioxidant capacity. Compared to the unencapsulated AP, SCAL exhibited a higher bioaccessibility of AP in mango juice, with a rapid release of AP during intestinal digestion. The pH values, total soluble solids, and colour properties of juice with SCAL did not change remarkably during juice storage at 4 °C for 28 days. On day 28, the retention of AP content and antioxidant capacity were higher in mango juice added with SCAL than the unencapsulated AP. Therefore, SCAL can be promising in delivering AP in aqueous food systems, making it possible to develop functional foods.

Polyelectrolyte-coated liposomes microfluidically assembled in one-step for enhancing cell endocytosis and in-vivo immune responses

To enhance the cellular uptake of liposomes, we prepared conventional liposomes with targeting molecules and surface-charged liposomes and evaluated their potential as nano-carriers and vaccine adjuvants by comparing their endocytosis efficiencies using immune cells. Surface-charged liposomes were synthesized via a one-step microfluidic method, which provided a novel, simple, fast, and highly reproducible method for preparing liposomes. Flow cytometry revealed that cationic polyelectrolyte-coated liposomes exhibited higher endocytosis efficiencies (of up to a factor of 100) in A774A.1 cells and JAWs II cells compared with uncoated liposomes or those coated with anionic polyelectrolytes. Positively charged liposomes exhibited some cytotoxicity at quaternary-chitosan coating concentrations higher than 6 mg/mL; however, significantly lower cytotoxicities (by a factor of almost ten) were obtained by protein mixing. Furthermore, BALB/c mice vaccinated with a mixture of Anthrax vaccine adsorbed (AVA) and quaternary chitosan-coated liposomes showed faster and stronger anti-PA IgG inductions compared to those vaccinated with AVA alone, with titers positively correlating with the amount of cationic liposome used. This finding clearly reveals that quaternary chitosan-coated liposomes act as both nano-carriers and vaccine adjuvants that significantly enhance in-vivo immune responses to vaccines with low immunogenicities.

Chitosan-coated liposome with lysozyme-responsive properties for on-demand release of levofloxacin

As an anti-infection antibiotic delivery route, a drug-controlled release system based on a specific condition stimulus response can enhance drug stability and bioavailability, reduce antibiotic resistance, achieve on-demand release and improve targeting and utilization efficiency. In this study, chitosan-coated liposomes containing levofloxacin (Lef@Lip@CS) were prepared with lysozyme in body fluids serving as an intelligent “switch” to enable accurate delivery of antibiotics through the catalytic degradation ability of chitosan. Good liposome encapsulation efficacy (64.89 ± 1.86 %) and loading capacity (5.28 ± 0.18 %) were achieved. The controlled-release behavior and morphological characterization before and after enzymatic hydrolysis confirmed that the levofloxacin release rate depended on the lysozyme concentration and the degrees of deacetylation of chitosan. In vitro bacteriostatic experiments showed significant differences in the effects of Lef@Lip@CS before and after enzyme addition, with 6-h inhibition rate of 72.46 % and 100 %, and biofilm removal rates of 51 % and 71 %, respectively. These findings show that chitosan-coated liposomes are a feasible drug delivery system responsive to lysozyme stimulation.

Liposomes Coated with Novel Synthetic Bifunctional Chitosan Derivatives as Potential Carriers of Anticancer Drugs.

In this study, liposomes coated with novel multifunctional polymers were proposed as an innovative platform for tumor targeted drug delivery. Novel Folic acid-Cysteine-Thiolated chitosan (FTC) derivatives possessing active targeting ability and redox responsivity were synthesized, characterized, and employed to develop FTC-coated liposomes. Liposomes were characterized for size, surface charge and drug encapsulation efficiency before and after coating. The formation of a coating layer on liposomal surface was confirmed by the slight increase in particle size and by zeta-potential changes. FTC-coated liposomes showed a redox-dependent drug release profile: good stability at physiological conditions and rapid release of liposome-entrapped calcein in presence of glutathione. Moreover, the uptake and cytotoxic activity of doxorubicin-loaded FTC-coated liposomes was evaluated on murine B16-F10 and human SKMEL2 melanoma cancer cells. Results demonstrated enhanced uptake and antitumor efficacy of FTC-coated liposomes compared to control chitosan-coated liposomes in both cancer lines, which is attributed to higher cellular uptake via folate receptor-mediated endocytosis and to triggered drug release by the reductive microenvironment of tumor cells. The proposed novel liposomes show great potential as nanocarriers for targeted therapy of cancer.

Novel Chitosan-Coated Liposomes Coloaded with Exemestane and Genistein for an Effective Breast Cancer Therapy.

For achieving high effectiveness in the management of breast cancer, coadministration of drugs has attracted a lot of interest as a mode of therapy when compared to a single chemotherapeutic agent that often results in reduced therapeutic end results. Owing to their proven effectiveness, good patient compliance, and lower costs, oral anticancer drugs have received much attention. In the present work, we formulated the chitosan-coated nanoliposomes loaded with two lipophilic agents, namely, exemestane (EXE) and genistein (GEN). The formulation was prepared using the ethanol injection method, which is considered a simple method for getting the nanoliposomes. The formulation was optimized using Box-Behnken design (BBD) and was extensively characterized for particle size, ζ-potential, Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) analysis. The sizes of conventional and coated liposomes were found to be 104.6 ± 3.8 and 120.3 ± 6.4 nm with a low polydispersity index of 0.399 and 0.381, respectively. The ζ-potential of the liposomes was observed to be -16.56 mV, which changed to a positive value of +22.4 mV, clearly indicating the complete coating of the nanoliposomes by the chitosan. The average encapsulation efficiency was found to be between 70 and 80% for all prepared formulations. The compatibility of the drug with excipients and complete dispersion of the drug inside the system were verified by FTIR, XRD, and DSC studies. Furthermore, the in vitro release studies concluded the sustained release pattern following the Korsmeyer-Peppas model as the best-fitting model with Fickian diffusion. Ex vivo studies showed better permeation of the chitosan-coated liposomes, which was further confirmed by confocal studies. The prepared chitosan-coated liposomes showed superior antioxidant activity (94.56%) and enhanced % cytotoxicity (IC50 7.253 ± 0.34 μM) compared to the uncoated liposomes. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay displayed better cytotoxicity of the chitosan-coated nanoliposomes compared to the plain drug, showing the better penetration and enhanced bioavailability of drugs inside the cells. The formulation was found to be safe for administration, which was confirmed using the toxicity studies performed on an animal model. The above data suggested that poorly soluble lipophilic drugs could be successfully delivered via chitosan-coated liposomes for their effective delivery in breast cancer.

Liposomal formulations of Oleae europaea L.: analyzing the antioxidant and antidiabetic activities along with toxicity profile in pancreatic beta TC6 cell line

ABSTRACT Olea europaea L. (Oleaceae), is rich in phenolic content and has powerful antioxidant and antidiabetic activity. However, there are no medicinal products prepared due to this feature. Therefore, this study aims to characterize an O. europaea extract with strong antioxidant and antidiabetic properties and to prepare nanoformulations containing this extract. To determine the activities of the extracts prepared from the leaves of the plant, DPPH• and ABTS•+ scavenging, Fe+3 reducing activity, α-amylase, and α-glucosidase inhibition assays were performed. The oleuropein content of the absolute ethanol extract with the highest activity was analysed by HPLC. The characterized extract was loaded into liposomes and chitosan coated liposomes, and the long-term sustainability of their activity was investigated. The encapsulation efficiency was 65.2% for the liposome and 66.8% for the chitosan-coated liposome formulation. The amounts of the extracts released from the formulations were evaluated to exhibit antioxidant and antidiabetic activity.

Preparation and Characterization of Novel Polyelectrolyte Liposomes Using Chitosan Succinate Layered over Chitosomes: A Potential Strategy for Colon Cancer Treatment.

Chitosan succinate is distinguished by its ability to shield the loaded drug from the acidic environment, localize and keep the drug at the colon site, and release the drug over an extended time at basic pH. The current study attempts to develop polyelectrolyte liposomes (PEL), using chitosan and chitosan succinate (CSSC), as a carrier for liposomal-assisted colon target delivery of 5 fluorouracil (5FU). The central composite design was used to obtain an optimized formulation of 5FU-chitosomes. The chitosan-coated liposomes (chitosomes) were prepared by thin lipid film hydration technique. After that, the optimized formulation was coated with CSSC, which has several carboxylic (COOH) groups that produce an anionic charge that interacts with the cation NH2 in chitosan. The prepared 5FU-chitosomes formulations were evaluated for entrapment efficiency % (EE%), particle size, and in vitro drug release. The optimized 5FU-chitosomes formulation was examined for particle size, zeta potential, in vitro release, and mucoadhesive properties in comparison with the equivalent 5FU-liposomes and 5FU-PEL. The prepared 5FU-chitosomes exhibited high EE%, small particle size, low polydispersity index, and prolonged drug release. PEL significantly limited the drug release at acidic pH due to the deprotonation of carboxylate ions in CSSC, which resulted in strong repulsive forces, significant swelling, and prolonged drug release. According to a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay, PEL treatment significantly decreased the viability of HT-29 cells. When compared to 5FU-liposome and 5FU-chitosome, the in vivo pharmacokinetics characteristics of 5FU-PEL significantly (p < 0.05) improved. The findings show that PEL enhances 5FU permeability, which permits high drug concentrations to enter cells and inhibits the growth of colon cancer cells. Based on the current research, PEL may be used as a liposomal-assisted colon-specific delivery.

Chondroitin sulfate and chitosan-coated liposomes as a novel delivery system for betanin: Preparation, characterization and in vitro digestion behavior

Betanin, a water-soluble pigment known for its high bioactivity, is hindered by pH and temperature sensitivity, weak ionic strength, and low bioavailability. In this study, nanoliposome (NPS), chitosan-coated NPS (CNPS), and chondroitin sulfate-chitosan bilayer-modified nanoliposomes (SCNPS) were prepared based on a layer-by-layer electrostatic interaction method for betanin encapsulation. The increase of polymer layers from NPS to SCNPS led to a monotonic increment from 223.57 to 522.33 nm in size, from −27.73 to 16.70 mV in negative charge and from 0.22 to 0.35 in polydispersity index. The chemical stability against pH (ranging from 2 to 10), ionic type (KCl, CaCl2, ALCl3) and ionic strength (100, 500 mM) significantly impacted the appearance and particle size of the double-layered nanoliposome. In vitro digestion experiment showed that SCNPS displayed higher stability and slower betanin release compared to NPS and CNPS. This study demonstrates that betanin can be efficiently encapsulated by SCNPS with improved stability and bioavailability.

Biophysical analysis on molecular interactions between chitosan-coated sinapic acid loaded liposomes and mucin

BackgroundThe mucus biomembrane is a primary barrier in delivering drugs to the brain via intranasal delivery. The negatively charged nanoformulations suffer from poor mucoadhesive ability and less retention time in the nasal cavity, which limits further therapeutic efficacy. The positively charged chitosan coating on liposomes may overcome the above issues. Hence, understanding the molecular interactions between the chitosan-coated liposomes and mucin is essential for developing an effective drug delivery system. MethodsThe molecular interactions of mucin with sinapic acid-loaded liposomes (SA-LPs) and mucin with chitosan-coated sinapic acid-loaded liposomes (SA-CH-LPs) were assessed using different biophysical instrumental analyses by interpreting the UV–Vis spectra and observing the particle size, polydispersity index, surface charge, and rheological behavior. ResultsThe mucin interaction with SA-CH-LPs showed increased viscosity as compared to SA-LPs with mucin. Moreover, the mucin interaction with SA-CH-LPs showed stronger mucoadhesive properties as compared to SA-LPs with mucin. The electrostatic interaction between positively charged SA-CH-LPs and negatively charged mucin was responsible for the enhanced mucoadhesive property. ConclusionThe positively charged SA-CH-LPs highly interact with mucin as compared to negatively charged SA-LPs. The mucoadhesive property of SA-CH-LPs could improve the retention of SA in the nasal cavity as compared to SA-LPs. These findings emphasize the importance of chitosan in modulating the mucoadhesive behavior of liposomes. General significanceOverall, this study helps to understand the molecular interactions and mucoadhesive nature of the chitosan-coated liposomes with mucin, which is essential for biological activity in the physiological environment.

Stability and cytotoxicity of biopolymer-coated liposomes for use in the oral cavity

This study investigates the stability and cytotoxicity of biopolymer-coated liposomes for use in the oral cavity. Liposomes (3 mM and 6 mM) were prepared by the thin film method and hydrated with phosphate buffer (PB) or glycerol phosphate buffer (G-PB). For coating, liposomes were added to a biopolymer solution of opposite charge. Particle stability was evaluated by measuring the size, polydispersity index, and zeta potential for up to 60 weeks. In vitro interaction of fluorescent-labelled biopolymer-coated liposomes and dysplastic oral keratinocytes was analyzed by confocal microscopy. Potential cytotoxicity was assessed in dysplastic oral keratinocytes by cell proliferation and cell viability. All three biopolymers showed good coating abilities for both concentrations and hydration media. The alginate coated liposomes in PB, 3 mM chitosan-coated liposomes in PB, and chitosan-coated liposomes in G-PB were stable for up to 60 weeks. In vitro studies demonstrated low cytotoxicity for all coated liposomes and non-specific cellular uptake of biopolymer-coated liposomes, independent of biopolymer, surface charge, lipid concentration and hydration media. All three formulations demonstrated low cytotoxicity and were considered safe. Alginate- and chitosan-coated liposomes demonstrated good stability over time and may be promising agents for use in the oral cavity and should be investigated further.

Fabricating pectin and chitosan double layer coated liposomes to improve physicochemical stability of beta-carotene and alter its gastrointestinal fate

To improve storage stability and gastrointestinal (GI) stability of liposomes, pectin and chitosan double layer coated liposome (P-C-L) was proposed and optimized using electrostatic deposition technique. The physical-chemical properties and GI fate of the carrier were then investigated in comparison to that of chitosan coated liposomes (C-L) and un-coated liposomes (L). The results showed P-C-L was successfully prepared at 0.2 % chitosan and 0.06 % pectin. It was hydrogen bonds between the amino groups in chitosan and liposomal interfacial region, and the interaction between the carboxyl groups in pectin layer and amino groups in chitosan layer maintained the structure of P-C-L after absorption by electrostatic interaction. The double layer coatings could improve chemical stability of the encapsulated β-carotene (βC), as well as the thermal stability of liposomes. What's more, the permeability of liposomal bilayers and βC release mechanism in simulated GI fluids was changed by the polymer coating. P-C-L exhibited better controlled release for βC than C-L and L, and displayer beneficial effect on delivering bioactive agents passing through intensity tract. This may assistant developing more efficient delivery system for bioactive agent.

Encapsulation of Hydrophobic Apigenin into Small Unilamellar Liposomes Coated with Chitosan Through Ethanol Injection and Spray Drying

Despite the multiple health benefits, natural flavonoid apigenin has poor aqueous solubility that restricts its delivery in foods. This study investigated the potential of spray-dried chitosan-coated liposomes prepared from scalable methods for the food industry as the delivery carriers for apigenin. Apigenin-loaded small unilamellar liposomes produced from ethanol injection had an encapsulation efficiency of 74.88 ± 5.31%. They were electrostatically stabilised via chitosan coating (0.25% w/v) and spray-dried. Spray-dried chitosan-coated apigenin liposomes (SCAL) exhibited the following powder characteristics: yield 66.62 ± 3.08%, moisture content 4.33 ± 0.56%, water activity 0.2242 ± 0.0548, particle size 10.97 ± 1.55 μm, nearly spherical morphology with wrinkles and dents under microscopic observation. Compared with the unencapsulated apigenin, SCAL demonstrated improved aqueous solubility (10.22 ± 0.18 mg/L), higher antioxidant capacity, and stability against simulated gastrointestinal digestion. The chitosan coating gave a slower in-vitro release of apigenin in SCAL (77.0 ± 6.2%) than that of uncoated apigenin liposomes (94.0 ± 5.3%) at 12 h. The apigenin release kinetics from SCAL could be represented by the Korsmeyer-Peppas model (R2 = 0.971). These findings suggest that SCAL could be a promising delivery system of apigenin for functional food applications.

Glycyrrhizic acid delivery system Chitosan-coated liposome as an adhesive anti-inflammation.

Nowadays, medicinal plants are used to overcome the side effects of prescription drugs in modern medicine. Glycyrrhizic acid (GA) derived from the root of the licorice plant is one of the plant compounds whose effectiveness has been confirmed in the treatment of inflammatory bowel disorders (IBD). Liposome thin film hydration method was used to synthesize chitosan-coated liposomes containing GA. In the present study, chitosan-coated liposome was characterized by dynamic light scattering (DLS), zeta potential, scanning electron microscope (SEM) and Fourier transforms infrared spectroscopy (FTIR). The FTIR spectrum confirmed the coating of liposomes by chitosan polymer. Liposome coating leads to an increase in the size and values of zeta potential. The 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay of chitosan-coated liposomes containing GA confirmed that it has no cytotoxicity toward fibroblasts cell line, therefore confirming their cytocompatibility. Overall, drug loading, release and cytotoxicity were evaluated and it was found that chitosan decreased the release rate of GA. It seems; chitosan-coated liposomes may be a suitable system for delivering liposomal GA in the treatment of IBD.

Lubricating Performance of Polymer-Coated Liposomes

Dry mouth is a troublesome condition linked to lubrication failure and leads to other diseases such as fungal infections and wounds in the oral cavity. There are many commercial salivary substitutes in the market, but none with a long-lasting lubrication effect. Polymer-coated liposomes can be an interesting formulation strategy for retrieving the symptoms of dry mouth by mimicking the micelles of saliva. In the present study, polymer coated-liposomes were prepared by the conventional thin film method and subsequently coated with three different polymers with different charge densities; alginate, chitosan and hydrophobically modified ethyl hydroxyethyl cellulose (HM-EHEC). The prepared polymer-coated liposomes were studied concerning their lubricating properties using a ball-on-disc tribometer at 2 N load at 37 °C, and their flow behaviours were also measured. Solutions of the pure polymers and dispersions of the uncoated liposomes were also studied to investigate any contributions from the individual components. A commercial dry mouth product based on HEC (hydroxyethyl cellulose) and glycerol was also included. The formulations were measured as soon as possible after preparation and some of them after >4 weeks. Results demonstrated that all the positively-charged formulations (chitosan, positive liposomes and chitosan-coated liposomes) had superior lubricating properties with friction coefficients (μ < 0.1) at orally relevant speeds (50 mm/s) as compared to the neutral or negatively-charged systems. At boundary lubrication conditions (3 mm/s), the chitosan-coated liposomes obtained an even lower friction force than the individual components, thus indicating a synergistic effect between the polymer and the liposome.

Chitosan-coated liposomes of Carrisa spinarum extract: synthesis, analysis and anti-pneumococcal potency

In the present study, a chitosan (CS)-coated liposome (LipCsP-Chitosan) nanocarrier was fabricated for the delivery of Carissa spinarum (CsP) polyphenols to improve bioavailability and anti-pneumococcal potential against Klebsiella pneumoniae. LipCsP-Chitosan was synthesized by the ion gelation method and characterized by using a Malvern zetasizer and Fourier Transform Infrared (FTIR); CsP encapsulation and release kinetics were investigated. Anti-pneumococcal activity of the nanoformulations was accessed by agar-well diffusion and microdilution assays. LipCsP-chitosan exhibited a hydrodynamic size and zeta potential of 365.22 ± 0.70 nm and +39.30 ± 0.61 mV, respectively. CsP had an encapsulation efficiency of 81.5%. FTIR analysis revealed the interaction of the liposomes with chitosan and the CsP. A biphasic CsP release profile followed by a sustained release pattern was observed. LiPCsP-Chitosan presented a higher bioaccessibility of polyphenols in the simulated gastric phase (74.1% ± 1.3) than in the simulated intestinal phase (63.32% ± 1.00). LipCsP-chitosan had a relative inhibition zone diameter of 84.33% ± 2.51 when compared to CsP. At minimum inhibition concentration of 31.25 mg/mL, LipCsP-Chitosan reduced the viability of Klebsiella pneumoniae by 57.45% ± 3.76 after 24 h. The results obtained from the current study offer a new approach to the utilization of LipCsP-Chitosan as nanocarriers for candidate anti-pneumococcal agents.