文献类型：期刊文献

中文题名：β-环糊精星形聚合物负载苯丁酸氮芥性能

英文题名：β-Cyclodextrin Based Star-like Polymer for Loading Chlorambucil

作者：陈涛[1];黄婵[1]

机构：[1]华东理工大学材料科学与工程学院,上海市先进聚合物材料重点实验室,上海200237

年份：2018

卷号：39

期号：10

起止页码：2350

中文期刊名：高等学校化学学报

外文期刊名：Chemical Journal of Chinese Universities

收录：CSTPCD;;EI(收录号：20185206314661);Scopus;北大核心:【北大核心2017】；CSCD:【CSCD2017_2018】；

基金：国家重点研发计划项目(批准号:2017YFB0309301,2017YFB0309302);上海市自然科学基金(批准号:17ZR1407200)资助.

语种：中文

中文关键词：聚甲基丙烯酸N,N-二甲氨基乙酯;β-环糊精;苯丁酸氮芥;主客体相互作用

外文关键词：Poly(N,N-dimethylaminoethyl methacrylate);β-Cyclodextrin;Chlorambucil;Host-guest interaction

摘要：通过原子转移自由基聚合,以溴化改性β-环糊精为引发剂,合成了星形聚合物β-环糊精-聚甲基丙烯酸N,N-二甲氨基乙酯(β-CD-PDMAEMA).采用红外光谱和核磁共振氢谱确定了星形聚合物的结构.分别在乙醇和水介质中,以β-CD-PDMAEMA为载体负载抗癌药物苯丁酸氮芥(CLB).通过紫外吸收光谱分析比较了2种介质中β-CD-PDMAEMA对CLB的载药效率及在37℃、不同p H值下的体外释药性能,分析了释药机理.结果表明,与乙醇相比,以水为介质时CLB能更多地通过主客体作用进入星形聚合物内核β-CD的疏水空腔,从而有更高的载药率,药物突释期短、突释量少,具有持续、高效的释放性能.CLB的释放属于扩散控制机理,PDMAEMA臂的质子化程度影响释药速率和累积释药量,表现出明显的p H响应性,酸性环境更有利于CLB的释放.
Star-like polymer withβ-cyclodextrin core(β-CD)and poly(N,N-dimethylaminoethyl methacrylate)arms(PDMAEMA),β-CD-PDMAEMA,was synthesized by atom transfer radical polymerization using brominatedβ-CD as initiator.The structure of the polymer was determined by Fourier transform infrared spectrophotometer(FTIR)and 1H nuclear magnetie resonance(NMR).The polymer was used to load hydrophobic anticancer drug chlorambucil(CLB)in both ethanol and water.The loading efficiency of CLB and in vitro release performance and mechanism at 37℃in buffer solutions with various pH values were investigated by UV absorption spectroscopy.The results show that,compared to that in ethanol,the hydrophobic internal cavity ofβ-CD in the core of the star-like polymer includes more CLB in water,which leads to higher drug loading ratio,shorter and less burst release.The release of CLB from the star-like polymer follows the diffusion mechanism.The release rate and cumulative release amount of CLB are affected by the protonation degree of PDMAEMA arms,which results to pH responsive release behavior.The acidic condition is beneficial to more efficient and sustained release of CLB.