摘要
目的研制载万古霉素PLGA/CS缓释复式微球,考察微球的体外释放性能。方法应用复乳-固化挥发法制备载盐酸万古霉素PLGA/CS复式微球。利用扫描电镜(SEM)及激光粒度分析仪进行形貌观测,采用紫外分光光度法测定盐酸万古霉素含量,计算载药率和包埋率;评价载药微球的体外释放行为,测定药物在微球中的稳定性,通过体外药物释放实验考察复合微球化处理对盐酸万古霉素溶出度的影响,用抑菌实验检测盐酸万古霉素的抗菌能力。结果以聚乙烯醇为乳化剂制备载万古霉素PLGA/CS缓释复式微球,微球表面光滑、无孔隙,粒径在(252.3±5.3)μm,平均载药量在(3.12±0.78)%。平均包埋率(33.57±2.17)%,在盐酸万古霉素PLGA/CS缓释微球具有明显的药物释放作用,体外释放90 d的药物累计释放高达80%以上。结论载盐酸万古霉素PLGA/CS微球性质稳定,释放周期比较长,抑菌效果明显,符合理想的局部抗感染应用要求。
Objective Prepare load Vancornycin hydrochloride PLGA/CS Duplex microspheres, investi- gated Duplex microsphere external release performance. Methods Prepare the Vancomycin hydrochloride - loaded Poly lactic acid glycolic acid copolymer Vancomycin by the multiple emulsion, ese the SEM and HPLC to observe, use the UV spectrophotometer to measuring the PLGA content, calculate particle size distribution, encapsulation efficiency. Evaluate the Duplex microspheres in vitro release, determine the drug Stability in the mi- crospheres. Results Use the Antibacterial experiment to test the Vancomycin hydrochloride active against bacteria. Experimental study released composite microspheres of treatment on Vancomycin hydrochloride by disso- lution in vitro drug, use the polyvinyl alcohol as emulsifier to Prepare load Vancomycin hydrochloride PLGA/CS duplex microspheres, the surface is smooth and no gap, average particle size is（252.3 ± 5.3）mm, the average drug loading was （3.12 ± 0.78）%, with an average encapsulation efficiency （33.57 ± 2.17）%. Vancomycin hydrochloride PLGA/CS Duplex microspheres have obvious drug release action. In vitro drug release 90d cumu- lative release up to 80 %. Conclusion Prepare load Vancomycin hydrochloride PLGA/CS Duplex microspheres quality is stable, Release cycle is more long, antibacterial effect is obvious, With the ideal of topical anti - infective applications.
出处
《内蒙古医学杂志》
2015年第6期641-645,F0004,共6页
Inner Mongolia Medical Journal
基金
国家自然科学基金项目(编号:81260281)
关键词
盐酸万古霉素
PLGA
壳聚糖
复式微球
体外释放
vancomycin hydrochloride
PLGA
chitosan
Duplex mierospheres
in vitro release
