快速膜乳化法制备粒径均一的PLGA微球和微囊  

Preparation of Uniform Size PLGA Microparticles and Microcapsules by Premix Membrane Emulsification

作　　者：田瑞[1,2] 王连艳[1] 吴颉 张洁[1,4] 曾烨婧[1,5] 马光辉[1] 

机构地区：[1]中国科学院过程工程研究所生化工程国家重点实验室,北京100190 [2]中国科学院研究生院,北京100049 [3]国家生化工程技术研究中心,北京100190 [4]北京科技大学土木与环境工程学院,北京100083 [5]北京化工大学生命科学与技术学院,北京100029

出　　处：《过程工程学报》2009年第4期754-762,共9页The Chinese Journal of Process Engineering

基　　金：国家自然科学重点基金资助项目(编号:205036050);中国科学院重要方向性项目资助(编号:KJCX2.YW.MO2;KGCX2-YW-210-1)

摘　　要：以聚(乳酸-羟基乙酸)(PLGA)为膜材,采用快速膜乳化结合溶剂萃取法制备了胰高血糖素样肽-1(GLP-1)微囊,研究了PLGA分子量对药物装载率、药物活性和体外释放行为的影响.制备均一微球的优化条件为过膜压力1000kPa,过膜次数3次,外水相稳定剂聚乙烯醇浓度19g/L,油水体积比1:5.在此条件下,制备了粒径350nm左右、多分散系数小于0.050的载GLP-1的PLGA微囊,GLP-1包埋率达65%以上,活性保留达85%以上,药物体外释药可达20d.Glucagon-like peptide-1（GLP-1） loaded poly（lactic-co-glycolic acid）（PLGA） microspheres were prepared by premix membrane emulsification and solvent extraction method.The preparation conditions of PLGA microparticles were optimized with respect to particle size and size distribution.The final optimum conditions were as follows：transmembrane pressure 1000 kPa,transmembrane pass 3,concentration of poly（vinyl alcohol）（PVA） in external water phase 19 g/L and volume ratio of oil phase to external water phase 1：5.The prepared microparticles under the conditions showed perfect spherical geometry and suitable size distribution.Under these conditions,uniform-sized GLP-1 loaded PLGA microspheres with different molecular weights were successfully prepared,the average diameter was about 300 nm,GLP-1 encapsulation efficiency 65%,and bioactivity 85%.Subsequently,their drug release in vitro was tested in phosphate buffered saline（pH 7.4） for 20 d.

关 键 词：聚(乳酸-羟基乙酸) 微球 胰高血糖素样肽-1 微囊 包埋 

分 类 号：R944.5[医药卫生—药剂学]