PLGA包埋硫酸庆大霉素缓释微球制备及体外释放行为.docVIP

PLGA包埋硫酸庆大霉素缓释微球制备及体外释放行为 　【摘要】 以生物可降解乙交酯和丙交酯的无规共聚物(PLGA)为载体，将硫酸庆大霉素分散在PLGA的有机溶液中，采用复乳溶剂挥发法制备了药物缓释微球。研究搅拌速度、PLGA浓度、乳化剂浓度和硫酸庆大霉素溶液体积对微球粒径的影响，观察微球的表面形貌，测定微球粒径、粒径分布和包封率，评价载药微球的体外释放行为。结果表明，采用甲基纤维素为乳化剂制备的微球形态完整，中粒径为(130±30)μm，微球中硫酸庆大霉素的包封率均在36%以上，平均42%，最高达56%。硫酸庆大霉素/PLGA微球具有显著的药物缓释作用，体外释放30d的累积释药率达80%以上。 【关键词】 PLGA微球； 硫酸庆大霉素； 复乳溶剂挥发法； 体外释放 Preparation and in vitro release behavior of the gentamicin sulfate-encapsulated PLGA microspheres Tan Hong-xiang and Ye Jian-dong (Key Laboratory of Specially Functional Materials, Ministry of Education, School of Material Science and Engineering, South China University of Technology, Guangzhou 510641) ABSTRACT Poly (D,L-lactide-co-glycolide) (PLGA) biodegradable microspheres with gentamicin sulfate for the local treatment of microbial bone infection were prepared by double emulsion and solvent evaporation method and characterized were studied. The conditions of the microspheres preparation such as the volume of gentamicin sulfate, PLGA concentration in organic solvent, stirring speed, emulsifier concentration were discussed. The surface morphology of the as-prepared microspheres was observed by SEM. The mean diameter and drug content of microspheres were analyzed and the drug release performance in vitro was evaluated. The results indicated that the morphology of the as-prepared PLGA microspheres by using of methyl cellulose as the dispersant was intact with a mean diameter of (130±30) μm and the average and maximum encapsulation efficiency of gentamicin sulfate was up to 56%, respectively. The cumulative rate of drug-release over 30 days drug-release time was over 80%, which illustrated satisfactory sustained-release of the gentamicin sulfate encapsulated PLGA microsperes. KEY WORDS PLGA microsphere; Gentamicin sulfate; Double emulsion and solvent evaporation method; In vitro release 骨髓炎是临床常见的骨感染疾病，其治疗时间通常需要4～6周［1］。硫酸庆大霉素(gentamicin sulfate，GS)广泛应用于敏感菌引起的局部感染，最早应用于临床的局部载药系统是聚甲基丙烯酸甲酯(PMMA)庆大霉素珠［1］， 但是PMMA不能够降解，需要二次手术取出。近年来，一