PCL-g-PEI聚合物载药胶束的制备及其性能研究  

STUDY ON PREPARATION OF PCL-g-PEI COPOLYMER MICELLES AND ITS PROPERTIES

作　　者：赵倩[1] 薛荣[1] 张毅[1,2] 韩晓燕[1] ZHAO Qian XUE Rong ZHANG Yi HAN Xiaoyan(Tianjin Key Laboratory of Chemistry and Analysis of Chinese Materia Medica College of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine Tianjin 300193, China Department of Experimental Teaching, Tianjin University of Traditional Chinese Medicine Tianjin 300193, China)

机构地区：[1]天津中医药大学中药学院,天津市中药化学与分析重点实验室,天津300193 [2]天津中医药大学实验教学部,天津300193

出　　处：《离子交换与吸附》2017年第2期107-119,共13页Ion Exchange and Adsorption

基　　金：国家自然科学基金(81202921)

摘　　要：以苯甲醇(Bn OH)为引发剂,异辛酸亚锡[Sn(Oct)2]为催化剂,开环聚合制得不同臂长的聚己内酯(PCL)聚合物,并接枝不同分子量聚乙烯亚胺(PEI)得到一系列两亲性聚合物PCL-g-PEI,对该聚合物结构进行核磁、红外表征。采用染料增溶法检测该聚合物形成胶束的临界胶束浓度(CMC),并以该胶束作为药物载体用于共包载葫芦素B(Cuc B)和阿霉素(Dox)两种药物,考察其载药效果及体外释药性能。结果表明,该系列聚合物具有较小的CMC值,且该CMC值随着疏水端PCL的增长而减小;载药胶束对Cuc B、Dox具有较高的包封率和载药量,体外释放行为表明,PCL-g-PEI载药胶束具有良好的缓释性能,有望成为抗癌中药(Cuc B)与化疗药物(Dox)联合用药的新型药物载体。A series of amphiphilic block coplymers PCL-g-PEI were synthesized by ring opening polymerization by benzylalcohol BnOH as initiator and stannous octoate as catalyst. The structures were confirmed by 1H-NMR and FT-IR. Dye solubilization method was used to determine critical micelle concentration （CMC） of copolymers. Cucurbitacin B （Cuc B） and Doxorubicin （Dox） coentrapped polymer micelle were prepared and their pharmaceutial properties were examined. The experimental results showed that the CMC value decreased with the increase the PCL block length. The PCL-g-PEI micelles have a certain drug-loading capacity and the release of drug-loaded micelle in vitro was showed sustained, for which the micelle was expected to become the new drug carrier of the combination of the anti-cancer traditional Chinese medicine （Cuc B） and chemotherapy （Dox）.

关 键 词：两亲性聚合物 聚乙烯亚胺接枝聚己内酯 聚合物胶束 葫芦素B 阿霉素 

分 类 号：O648[理学—物理化学]