Li Jiaxin, Tang Ruimin, Zhang Penghao, Yuan Minglong, Li Hongli, Yuan Mingwei
National and Local Joint Engineering Research Center for Green Preparation Technology of Biobased Materials, Yunnan Minzu University, Kunming 650500, China.
J Funct Biomater. 2022 Aug 4;13(3):113. doi: 10.3390/jfb13030113.
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.
载药微球是一种理想的骨组织递送材料。在本研究中,一种可生物降解的席夫碱壳聚糖 - 聚丙交酯被用作包封材料,以制备载药微球,作为万古霉素控释的生物相容性载体。在此方面,通过席夫碱法制备席夫碱壳聚糖,然后通过开环聚合法制备不同比例的席夫碱壳聚糖 - 聚丙交酯聚合物。采用W/O乳液法制备载药微球,并通过核磁共振(NMR)、红外光谱(IR)和抗菌方法对聚合物和聚合物微球进行表征和研究。测定微球的载药量和释放速率,以研究不同比例下药物微球的载药量、包封率和释放速率。在本研究中,成功制备了不同比例的席夫碱壳聚糖 - 聚乳酸材料,并以它们为载体成功制备了载万古霉素微球。本研究证明这些材料对金黄色葡萄球菌和大肠杆菌具有抗菌活性。载药微球的粒径低于10μm,且粒径随分子量降低而减小。所得结果表明,1:100的微球具有最高的载药量和包封率,载药微球在24小时内无突释现象,释放量达到20%以上。释放30天后,1:10、1:20、1:40、1:60和1:100载药微球的释放量分别为64.80±0.29%、54.43±0.54%、44.60±0.43%、42.53±0.40%和69.73±0.45%,其中1:100的释放量最高。