4.6 Article

Alkylated chitosan nanomaterials for enhanced antimicrobial activity and delivery of fusidic acid: Preparation and preliminary in vitro investigation

Journal

JOURNAL OF APPLIED POLYMER SCIENCE
Volume 140, Issue 26, Pages -

Publisher

WILEY
DOI: 10.1002/app.53990

Keywords

chitosan; fusidic acid; nanomaterials; percutaneous delivery; polymer alkylation

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The study investigates the fabrication of nanomaterials made of amphiphilically-altered polysaccharides and their potential in enhancing drug transport across the skin. Alkylated chitosan nanomaterials were constructed and compared with neat chitosan nanomaterials in terms of drug release and diffusion. The results demonstrate that alkylated chitosan nanomaterials exhibit slower drug release but faster penetration across the skin, and have better antimicrobial activity.
Nanomaterials manufactured of amphiphilically-altered polysaccharides have sparked a great deal of interest due to their capability to elevate drug transport across the skin. The study presents the fabrication of alkylated chitosan through 2-tert-butoxymethyloxirane alteration (alkylation degree 29.7%), that was typified by spectroscopic, chromatographic, and thermal analysis approaches before being constructed into nanomaterials for the analysis of their capability in governing fusidic acid diffusion percutaneously. The nanomaterials were constructed via the ionic interaction of positively charged chitosan and negatively charged cross linker sodium tripolyphosphate, with a loading degree of fusidic acid of ca. 20% reported. Fusidic acid release was slower in nanomaterials constructed of alkylated chitosan than in neat chitosan. Under application-relevant conditions, in vitro incubation with HaCaT cells exhibited insignificant toxicity. Using Franz diffusion cells, the alkylated chitosan nanomaterials induced fusidic acid to infiltrate the Strat-M (R) membrane at a 2-fold greater rate than the neat chitosan nanomaterials. Based on the agar diffusion test, fusidic acid was shown to have better antimicrobial activity when loaded into alkylated chitosan nanomaterials than when loaded into neat chitosan nanomaterials. Ultimately, the in vitro results revealed that alkylated chitosan nanomaterials offer a great deal of potential for percutaneous delivery, which merits greater analysis.

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