The Preparation and Characterization of Chitooligosaccharide–Polylactide Polymers, and In Vitro Release of Microspheres Loaded with Vancomycin

Abstract

Drug-loaded microspheres are an ideal bone tissue delivery material. In this study, a biodegradable Schiff base chitosan–polylactide was used as the encapsulation material to prepare drug-loaded microspheres as biocompatible carriers for controlled vancomycin release. In this regard, Schiff base chitosan was prepared by the Schiff base method, and then different proportions of the Schiff base chitosan–polylactide polymer were prepared by ring-opening polymerization. Drug-loaded microspheres were prepared by the W/O emulsion method, and the polymers and polymer microspheres were characterized and studied by NMR, IR, and antibacterial methods. The drug loading and release rates of microspheres were determined to investigate the drug loading, encapsulation efficiency, and release rate of drug microspheres at different ratios. In this study, different proportions of Schiff base chitosan–polylactic acid materials are successfully prepared, and vancomycin-loaded microspheres are successfully prepared using them as carriers. This study proves that the materials have antibacterial activities against Staphylococcus aureus and Escherichia coli. The particle size of drug-loaded microspheres was below 10 μm, and the particle size decreased with decreasing molecular weight. The obtained results show that 1:100 microspheres have the highest drug-loading and encapsulation efficiencies, the drug-loaded microspheres have no burst release within 24 h, and the release quantity reaches more than 20%. After 30 days of release, the release amounts of 1:10, 1:20, 1:40, 1:60, and 1:100 drug-loaded microspheres were 64.80 ± 0.29%, 54.43 ± 0.54%, 44.60 ± 0.43%, 42.53 ± 0.40% and 69.73 ± 0.45%, respectively, and the release amount of 1:100 was the highest.