顺铂-聚己内酯微球的研制及其缓释性能测试  

Preparation of Cisplatin-loaded Polycaprolactone Microspheres and Their Sustained Release Performance

作　　者：林爱珠 方芳 吴宏霞[3] 刘天惠 柯方[1] 林媚[1] LIN Aizhu;FANG Fang;WU Hongxia;LIU Tianhui;KE Fang;LIN Mei(Department of medicinal chemistry,School of Pharmacy,Fujian Medical University,Fuzhou 350122,China;Fujian Provincial Institute of Dermatology and Venereology,Fuzhou 350009,China;Center for Comprehensive Experimental Pharmacy,Fujian Medical University,Fuzhou 350122,China)

机构地区：[1]福建医科大学药学院药物化学系,福州350122 [2]福建省皮肤病性病防治院,福州350009 [3]福建医科大学药学院实验中心,福州350122

出　　处：《福建医科大学学报》2019年第4期219-223,共5页Journal of Fujian Medical University

基　　金：福建省自然科学基金(2015J01316;2016J01686);福建省科技创新联合资金(2016Y9053)

摘　　要：目的制备顺铂-聚己内酯微球,探讨该微球载药量、粒径大小及体外释放的影响因素。方法采用水包油(O/W)乳化法和溶剂挥发相结合的方法制备微球,利用紫外分光光度计测定载药率和包封率,采用偏光显微镜及扫描电镜观察其粒径大小和表面形态。结果当聚乙烯醇浓度为3.5%、乳化搅拌速度为800 r/min时,采用高分子量的聚己内酯负载顺铂,可制得粒径约为54μm的顺铂微球,其载药率为7.8%、顺铂包封率为75%。药物释放速率与微球粒径大小有关,且遵循Fickian扩散定律。结论通过优化条件制得的顺铂聚己内酯微球形态良好,粒径均一,有良好的缓释行为。ObjectiveTo prepare cisplatinloaded polycaprolactone microspheres and investigate the influencing factors on drugloading rate,particle size and sustained release property.MethodsThe microspheres were fabricated by oilinwater(O/W)emulsion and solvent evaporation technique.The drug loading rate and encapsulation efficiency of microspheres were investigated by using ultraviolet spectrophotometry(UV)and the shape and particles size of microspheres were characterized by polarizing microscope and scan electron microscope(SEM).ResultsThe results showed that cisplatinloaded microspheres of 54μm size were prepared with high molecular weight of polycaprolactone when the concentration of polyvinyl alcohol was 3.5%and the speed of emulsification was 800 r/min.The drug loading rate could reach 7.8%and the encapsulation efficiency of cisplatin could reach about 75%.The drug release behavior of microspheres was related to the size of microspheres and fitted well with the Fickian diffusion model.ConclusionThe resulting cisplatinloaded microspheres has good shape,homogeneous particle size and good sustained release properties under the optimized conditions.

关 键 词：顺铂 聚合物 内酯类 微球体 迟效制剂 

分 类 号：R318.08[医药卫生—生物医学工程] R944.9[医药卫生—基础医学]