Evaluation of micellar architecture based on functionalized chitosan for the in vitro release of an antibiotic

Abstract

Polymeric micelles are enjoying high resurgence of interest in biomedical field as promising candidates for the delivery of water-insoluble drugs. This property was used to design and synthesize fatty acid grafted polysaccharide-based copolymer micelles for the sustained release of Cefixime trihydrate (CFX): a third-generation cephalosporin. Chitosan (CS), a polysaccharide obtained by the alkaline deacetylation of chitin emerged as a useful drug delivery matrix because of its polycationic nature, biodegradability, biocompatibility and mucoadhesiveness. The drug release was monitored in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (7.4). The in vitro release studies revealed 52% of drug release after 24 h of incubation and were enhanced to 83% after 72 h in simulated intestinal fluid condition. Antibacterial studies confirmed that the inherent properties of the drug were retained as well as enhanced by micelle formation. Thus, the synthesized copolymer micelle assures to be an excellent carrier vehicle for the sustained release of a model hydrophobic drug CFX. Smaller particle size ensures increased drug uptake and controlled release facilitates patient compliance.