二硫键链接的两亲性嵌段合物的合成及胶束化研究  

Synthesis and micellization of amphiphilic block copolymers with disulfide bond

作　　者：姚琳[1] 余丽丽[1] 梁飞[1] 尤静[1] 张隽荣 宁梓任 

机构地区：[1]西安医学院药学院,陕西西安710021

出　　处：《化工科技》2016年第5期11-15,共5页Science & Technology in Chemical Industry

基　　金：国家自然科学基金青年基金资助项目(81302706);国家级大学生创新创业训练计划项目(201411840009);陕西省大学生创新创业训练计划项目(2301);陕西省大学生创新创业训练计划项目(2302)

摘　　要：通过二硫吡啶基活化的聚乙二醇与巯基聚己内酯之间的偶联反应,在聚乙二醇单元与聚己内酯单元间引入二硫键,合成二嵌段共聚物mPEG-SS-PCL,通过核磁氢谱和红外光谱等手段对聚合物的结构进行表征。以阿霉素(DOX)为药物模型,通过紫外分光光度法分析了聚合物对脂溶性药物的包载能力,用激光粒度仪测定胶束粒径、粒径分布。结果表明,空白胶束及载药胶束的平均粒径分别为117.7nm和146.1nm,该聚合物对阿霉素具有良好的药物包载能力,最高载药量为16.28%,包封率为54.26%。After seven steps of reaction,a new disulfide-linked diblock copolymer of mPEG and PCL（mPEG-SS-PCL）was synthesized,which was repared by introducing a disulfide bond between pyridyl disulphide activated polyethylene glycol（mPEG-SS-Py）and mercapto polycaprolactone（PCL-SH）by the coupling reaction.Structure of polymers was characterized by -1H NMR,FT-IR and other methods.The carrying capacity of the polymer for lipophilic drugs was analyzed by UV spectrophotometry using adriamycin（DOX）as the model drug.The particle size and particle size distribution of the micelles were determined by laser particle size analyzer.The average particle sizes of the micelles and drug loaded micelles were 117.7nm and 146.1nm respectively.This polymer has better drug loading capacity for DOX.The highest drug loading capacity was 16.28%,and the encapsulation efficiency was 54.26%.

关 键 词：两亲性聚合物 二硫键 偶联反应 

分 类 号：O633.3[理学—高分子化学]