The Analysis of Chitosan-Coated Nanovesicles Containing Erythromycin—Characterization and Biocompatibility in Mice

Hilițanu, Loredana Nicoleta; Mititelu-Tarțău, Liliana; Popa, Grațiela; Buca, Beatrice Rozalina; Pavel, Liliana Lacramioara; Pelin, Ana-Maria; Meca, Andreea-Daniela; Bogdan, Maria; Pricop, Daniela

doi:10.3390/antibiotics10121471

Cited by 6 publications

(3 citation statements)

References 44 publications

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“…Furthermore, Hilițanu et al confirmed the biocompatibility of chitosan-coated liposomes containing erythromycin after oral administration in mice. The authors investigated erythrocyte counts, liver enzyme activity, serum urea plasma levels, immunological biomarkers, and histopathological examinations of liver or kidney, and found no significant changes in the mice ( Hilițanu et al, 2021 ).…”

Section: Resultsmentioning

confidence: 99%

Chitosan-based delivery system enhances antimicrobial activity of chlorhexidine

Hemmingsen

Panchai²,

Julin³

et al. 2022

Front. Microbiol.

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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.

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Section: Resultsmentioning

confidence: 99%

Chitosan-based delivery system enhances antimicrobial activity of chlorhexidine

Hemmingsen

Panchai²,

Julin³

et al. 2022

Front. Microbiol.

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“…A recent paper reported the preparation of liposomal ERY by an active loading technique method, followed by coating with chitosan [ 43 ]. The resulted liposomes showed a hydrodynamic diameter of 311 nm and an EE of 55%.…”

Section: Vesiclesmentioning

confidence: 99%

Erythromycin Formulations—A Journey to Advanced Drug Delivery

2022

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Erythromycin (ERY) is a macrolide compound with a broad antimicrobial spectrum which is currently being used to treat a large number of bacterial infections affecting the skin, respiratory tract, intestines, bones and other systems, proving great value from a clinical point of view. It became popular immediately after its discovery in 1952, due to its therapeutic effect against pathogens resistant to other drugs. Despite this major advantage, ERY exhibits several drawbacks, raising serious clinical challenges. Among them, the very low solubility in water and instability under acidic conditions cause a limited efficacy and bioavailability. Apart from this, higher doses promote drug resistance and undesirable effects. In order to overcome these disadvantages, during the past decades, a large variety of ERY formulations, including nanoparticles, have emerged. Despite the interest in ERY-(nano)formulations, a review on them is lacking. Therefore, this work was aimed at reviewing all efforts made to encapsulate ERY in formulations of various chemical compositions, sizes and morphologies. In addition, their preparation/synthesis, physico-chemical properties and performances were carefully analysed. Limitations of these studies, particularly the quantification of ERY, are discussed as well.

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“…Surface coating the vesicles with polymers leads to an increase in their stability, lengthening of their life in the blood stream, and offers sustained release of the contained medicine. The polymer chitosan was selected to coat the NSPs in order to target medications to maximize their absorption [ 21 ]. Chitosan, a natural polysaccharide derived from marine crustaceans, mollusks, insects, and fungi, is of great interest, particularly in drug delivery and biomedical application [ 22 , 23 ].…”

Section: Introductionmentioning

confidence: 99%

Formulation of Chitosan-Coated Brigatinib Nanospanlastics: Optimization, Characterization, Stability Assessment and In-Vitro Cytotoxicity Activity against H-1975 Cell Lines

et al. 2022

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The purpose of the current study was to develop Brigatinib (BGT)-loaded nanospanlastics (BGT-loaded NSPs) (S1-S13) containing Span 60 with different edge activators (Tween 80 and Pluronic F127) and optimized based on the vesicle size, zeta potential (ZP), and percent entrapment efficiency (%EE) using Design-Expert® software. The optimum formula was recommended with desirability of 0.819 and composed of Span-60:Tween 80 at a ratio of 4:1 and 10 min as a sonication time (S13). It showed predicted EE% (81.58%), vesicle size (386.55 nm), and ZP (−29.51 mv). The optimized nanospanlastics (S13) was further coated with chitosan and further evaluated for Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), in vitro release, Transmission Electron Microscopy (TEM), stability and in-vitro cytotoxicity studies against H-1975 lung cancer cell lines. The DSC and XRD revealed complete encapsulation of the drug. TEM imagery revealed spherical nanovesicles with a smooth surface. Also, the coated formula showed high stability for three months in two different conditions. Moreover, it resulted in improved and sustained drug release than free BGT suspension and exhibited Higuchi kinetic release mechanism. The cytotoxic activity of BGT-loaded SPs (S13) was enhanced three times in comparison to free the BGT drug against the H-1975 cell lines. Overall, these results confirmed that BGT-loaded SPs could be a promising nanocarrier to improve the anticancer efficacy of BGT.

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The Analysis of Chitosan-Coated Nanovesicles Containing Erythromycin—Characterization and Biocompatibility in Mice

Cited by 6 publications

References 44 publications

Chitosan-based delivery system enhances antimicrobial activity of chlorhexidine

Chitosan-based delivery system enhances antimicrobial activity of chlorhexidine

Erythromycin Formulations—A Journey to Advanced Drug Delivery

Formulation of Chitosan-Coated Brigatinib Nanospanlastics: Optimization, Characterization, Stability Assessment and In-Vitro Cytotoxicity Activity against H-1975 Cell Lines

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