pH响应性聚合物胶束的制备、表征及对阿霉素的控制释放研究  

pH-sensitive polymeric micelles:preparation,characterization and controlled release of DOX

作　　者：苑莹芝 马敏[1] 张丹[1] 袁建超[1] 

机构地区：[1]西北师范大学化学化工学院,甘肃省高分子材料重点实验室,甘肃兰州730070

出　　处：《化学研究》2016年第5期630-635,共6页Chemical Research

基　　金：国家自然科学基金资助项目(21364011,20964003)

摘　　要：以主链含腙键的聚乙二醇大分子（PEG-NH-N=CH-OH）为引发剂,通过开环聚合己内酯（ε-CL）,制备了一种具有pH响应性的两亲性嵌段共聚物PEG-NH-N=CH-PCL.运用核磁共振（^1H NMR）、透射电镜（TEM）和动态光散射（DLS）等对聚合物的结构、胶束的形貌及粒径进行表征.结果表明,聚合物胶束呈规整球形且分布均匀,平均粒径约98nm,pH 5.0时胶束粒径显著增加.负载阿霉素（DOX）的聚合物胶束的载药量为16.4%,包封率为57.4%.体外释放研究表明,pH 5.0时药物释放速率比pH 7.4时快,48h后累计释放率达91.1%.因此,该pH响应性聚合物胶束作为抗癌药物载体具有潜在的应用价值.A novel pH-sensitive block copolymer（PEG-NH-N=CH-PCL）containing hydrazone bond was synthesized by ring-opening polymerization ofε-caprolactone（ε-CL）in the presence of PEG macromolecular initiator containing hydrazone bond（PEG-NH-N=CHOH）.The structure of polymer,morphology and particle size of micelles were confirmed by nuclear magnetic resonance（~1H NMR）,transmission electron microscopy（TEM）and dynamic light scattering（DLS）.The results showed that polymeric micelles had regular spherical structure and mean size was about 98 nm,the diameter of the micelles increased significantly in pH 5.0.The drug loading content and loading efficiency of DOX-loaded micelles were 16.4%and 57.4%,respectively.The in vitro release studies suggested that the drug release of micelles in pH 5.0was much faster than that in pH 7.4.The cumulative release rate was up to 91.1%within 48 h.Thus,the pH-responsive polymer micelles have potential applications as anti-cancer drug carrier.

关 键 词：聚合物胶束 两亲性嵌段共聚物 PH响应性 阿霉素 控制释放 

分 类 号：O63[理学—高分子化学] TB381[理学—化学]