基于主客体识别作用构筑的聚合物前药胶束及其药物控释性能研究  

Construction of polymeric prodrug micelles based on host-guest interaction and their drug control release behaviors

作　　者：刘彩萍 白阳 LIU Cai ping;BAI Yang(College of Chemistry and Chemical Engineering,Shaanxi Key Laboratory of Chemical Additives for Industry,Shaanxi University of Science ＆ Technology,Xi＇an 710021,China)

机构地区：[1]陕西科技大学化学与化工学院陕西省轻化工助剂重点实验室,陕西西安710021

出　　处：《陕西科技大学学报》2018年第4期63-70,共8页Journal of Shaanxi University of Science & Technology

基　　金：陕西省教育厅专项科研计划项目(17JK0103);陕西科技大学青年拔尖人才科研启动基金项目(2016QNBJ-10)

摘　　要：研究制备了一种基于超分子聚合物的pH响应性前药胶束,其主体分子是β-环糊精-阿霉素前药分子,客体分子为偶氮苯封端的聚甲基丙烯酸N,N-二甲氨基乙酯.利用二维核磁NOESY谱鉴定了环糊精与偶氮苯之间的主客体包合作用,利用动态光散射和透射电子显微镜表征了超分子聚合物胶束的形貌和尺寸.结果表明超分子聚合物在水溶液中形成了球形纳米胶束,其粒径尺寸在80~100nm.超分子聚合物-前药胶束体外药物控释行为具有pH响应特性,分别在pH5.0和pH7.4下研究了其对药物的控释行为.利用荧光光谱法测定药物分子DOX的累计释放率,结果表明连接抗癌药物DOX分子的酰腙键对酸性环境极为敏感,可在短时间内被还原,实现抗癌药物的有效释放.pH-sensitive supramolecular polymeric micelles were constructed by host-guest interactions betweenβ-CD-hydrazone-DOX and azobenzene terminated poly（2-（Dimethylamino）ethyl methacrylate）（Azo-PDMA）.The host-guest interactions betweenβ-cyclodextrin and azobenzene were investigated by 2 D NOESY spectroscopy,and the morphology and size of supramolecular polymer micelles were investigated by dynamic light scattering（DLS）and transmission electron microscopy（TEM）.On the basis of mentioned results,supramolecular micelles formed in the pure water possessed proper and uniform size（with diameters of 80~100 nm）.Finally,the drug control release behavior of these micelles was analyzed in pH5.0 and pH7.4 phosphate buffer solution respectively.Then the concentration of released DOX was determined by fluorescence spectrometry.The results suggested that the hydrazine bond can be responsive in acid environment,leading to the release of DOX in a short time.

关 键 词：PH敏感 超分子聚合物 聚合物胶束 主客体包合 

分 类 号：O6[理学—化学]