局部用雷帕霉素聚乳酸乙醇酸共聚物缓释微球制备及释药研究.docVIP

局部用雷帕霉素聚乳酸乙醇酸共聚物缓释微球制备及释药研究 　　[摘要]目的:介绍雷帕霉素(RAPA)聚乳酸乙醇酸共聚物(PLGA)缓释微球的制备方法,建立高效液相色谱法(HPLC)测定体系以检测微球中雷帕霉素含量,检测微球性状并进行体外释药实验。方法:以聚乳酸乙醇酸共聚物为载体,采用W/O/W 乳剂-扩散溶剂挥发法制备雷帕霉素缓释微球,扫描电镜检测微球外观及微球粒径,HPLC检测微球载药量、包封率及体外释药量。结果:所制微球光滑圆整,大小均一,平均粒径:(121.18±27.83)μm,载药率:(14.39 ± 1.32)%,包封率:(72.92±4.29)%,体外释放实验显示1～4天有突释,随后平稳释药至第10天累积释药率达80%。结论:采用制备工艺稳定,所制微球载药量及包封率均较高,形态完整,大小均一,体外释药较为平稳并且具有明显的缓释作用。 　　[关键词]雷帕霉素;缓释;微球;PLGA 　　[中图分类号]Q813.1[文献标识码]A[文章编号]1008-6455(2010)03-0334-04 　　 　　Preparation and in vitro release study of rapamycin in poly(lactic-co-glycolic )acid microsphere for topical administration 　　PEI Jiao-miao,XUE Xiao-yan,LIU Bei,XIA Wei,LUO Xiao-xing,GUO Shu-zhong 　　(Institute of Plastic Surgery of Peoples Liberation Army,Xijing Hospitol,the Fourth Military Medical University,Xian 710032,Shaanxi,China) 　　 　　Abstract:ObjectiveTo optimize the preparation technology of poly (lactide - co - glycolide) (PLGA) microspheres loaded with rapamycin (RAPA-PLGA-MS), establish a HPLC method for content determination of rapamycin in microspheres and study powder particle characteristics and in vitro release characteristics of RAPA-PLGA-MS. Methods RAPA-PLGA-MS was prepared with PLGA as carriers by the water-in-oil-in-water(W/O/W) emulsion solvent evaporation method. Scanning electron miroscope (SEM) and HPLC were used to evaluate the micromeritic characteristics of RAPA-PLGA-MS, such as the particle size,loading efficiency, and entrapment efficiency and in vitro release characteristics.ResultsThe prepared microspheres were spherical with smooth surfaces,with an average particle size of (121.18±27.83) μm. The loading and encapsulation efficiency were (14.39±1.32)% and (72.92±4.29)% respectively. The in vitro release curve of RAPA-PLGA-MS was up to 80% in 10 days.Conclusions Rapamycin poly(lactic-co-glycolic )acid microspheres was successfully prepared and has obvious sustained release. ???　Key words:rapamycin;controlled release;microspheres;PLGA 　　 　　随着显微外科技术的进步与推广以及抗免疫排斥药物的研发与改良,同种