两亲嵌段聚合物载药胶束的绿色制备技术  

Green synthesis method of drug-loaded micelles based on amphiphilic diblock copolymer

作　　者：焦真[1] 刘娜[1] 陈志明[1] 

机构地区：[1]东南大学化学化工学院,南京211189

出　　处：《东南大学学报（自然科学版）》2010年第5期1009-1012,共4页Journal of Southeast University：Natural Science Edition

基　　金：江苏省高技术研究计划资助项目(BG2006038)

摘　　要：为了避免制备过程中有机溶剂的使用,开发了一种两亲嵌段聚合物载药胶束的新型绿色制备法——超临界二氧化碳挥发法,在自制的实验装置中成功制备了聚(2-甲基丙烯酰氧乙基磷酰胆碱)-聚甲基丙烯酸正丁酯(PM PC-b-PBMA)载紫杉醇胶束.该胶束具有较规则的球形形貌和较小的粒径分布,平均粒径为54nm,药物的包封率和载药量分别为61.0%和12.2%,与有机溶剂挥发法制备的胶束相当.体外释药动力学研究结果表明,该胶束可在人体血液环境中平缓释药,132h内的释药量达到55%,远高于采用有机溶剂挥发法制得的胶束.超临界二氧化碳挥发法有望成为缓释药物体系的新型制备法.A novel green method for fabricating amphiphilic diblock copolymers micelles,the supercritical carbon dioxide evaporation method,is developed to avoid the usage of organic solvents during the preparation.The paclitaxel-loaded polymeric micelles composed of poly（n-butyl methacrylate）-b-poly（2-methacryloyloxyethyl phosphorylcholine）（PMPC-b-PBMA） are successfully prepared in a set of self-made equipment.The micelles have a regular spherical shape and a narrow size distribution.The mean diameter is 54nm.The drug encapsulation efficiency and the drug loading content of the micelles are 61.0% and 12.2%,respectively,which are similar to those of the micelles prepared by the organic solvent evaporation method.The results of the in vitro release kinetics study of paclitaxel from the micelles indicate that 55% of the paclitaxel is released from the micelles within 132h,which is much higher than the micelles prepared by the organic solvent evaporation method.Therefore,the supercritical carbon dioxide evaporation method has potential application in the preparation of controlled drug release systems.

关 键 词：超临界二氧化碳挥发法 两亲嵌段聚合物 紫杉醇 胶束 控制释药 

分 类 号：TQ469[化学工程—制药化工]