枝化-环化结构共聚物用于酸响应载药体系  

Synthesis of Branched Cyclic Copolymer for pH-responsive Drug Delivery System

作　　者：谢德彪 宋华杰 曹红亮[1] 陈新[1] XIE De-biao SONG Hua-jie CAO Hong-liang CHEN Xin(College of Material Science and Engineering, Key Laboratory for Ultra Fine Materials of Ministry of Education, Shanghai Key Laboratory of Advanced Polymer Materials,East China University of Science and Technology, Shanghai 200237, Chin)

机构地区：[1]华东理工大学材料科学与工程学院超细材料制备与应用教育部重点实验室,上海市先进聚合物材料重点实验室,上海200237

出　　处：《精细化工》2017年第10期1114-1118,1125,共6页Fine Chemicals

基　　金：上海市重点学科和重点实验室项目(B502,08DZ2230500);上海市浦江人才计划(13PJ1401700)~~

摘　　要：将溴代聚乙二醇(PEG2000Br)和缩醛化物二(2-丙烯酰氧基乙氧基)-(4-甲氧基苯基)甲烷(ACD)分别作为引发剂和单体,采用逆向增强原子转移自由基聚合(DE-ATRP)法得到嵌段共聚物聚乙二醇-b-聚[二(2-丙烯酰氧基乙氧基)-(4-甲氧基苯基)甲烷](PEG-b-PACDs)。通过核磁共振氢谱和凝胶渗透色谱表征了该聚合物的结构;用动态光散射和透射电镜表征了胶束的尺寸和形貌。结果表明,聚合物呈现枝化-环化结构,空白胶束的尺寸在70 nm左右,载药胶束尺寸在90 nm左右,胶束的药物包封率为48.7%。在pH为7.4时透析48 h后,药物释放率只有32.5%,在pH为5.4时透析48 h后,药物释放率为68.3%,表明共聚物在酸性条件下具有良好的药物缓释性。A branched cyclic amphiphilic block copolymer（ PEG-b-PACDs） was synthesized via a deactivation-enhanced atom transfer radical polymerization（ DE-ATRP） with brominated polyethylene glycol（ PEG2KBr） and di（ 2-acry-loyloxy ethoxy）-[4-methoxy-phenyl]methane（ ACD） as initiator and hydrophobic monomer,respectively. And then its potential application for a drug delivery system was explored. The structure of copolymer was characterized by means of hydrogen spectrum nuclear magnetic resonance（1HNMR） and gel permeation chromatography（ GPC）. The particle size and morphology of the micelles were measured by dynamic light scattering（ DLS） and transmission scanning microscope（ TEM）. The results showed that the resulting copolymer exhibited a branched cyclic structure. The blank micelles were spherical in shape with a particle size of 70 nm,while the particle size of doxorubicin（ DOX）-loaded micelles were about 90 nm. The encapsulation efficiencies of DOX-loaded micelles were 48. 7%. The DOX-loaded PEG-b-PACDs shows obvious pH-responsive drug release property under acidic condition.

关 键 词：纳米结构自组装 DE-ATRP PH响应性 嵌段共聚物 枝化-环化结构 功能材料 

分 类 号：TQ469[化学工程—制药化工]