酸敏感型两亲性聚合物的制备和释药性能研究  

Preparation and drug release properties of acidic sensitive amphiphilic polymers

作　　者：尤静[1] 余丽丽[1] 姚琳[1] 杨宽[1] 

机构地区：[1]西安医学院药学院,西安710021

出　　处：《化工新型材料》2014年第1期40-42,共3页New Chemical Materials

基　　金：国家自然科学基金青年基金(81302706);陕西省教育厅科研计划项目(2013JK0759);西安医学院博士科研启动基金(2011DOC05);西安医学院教师科研计划项目(12FZ04);西安医学院校级科研计划大学生科研项目(12DXS01);陕西省大学生创新创业训练计划项目(201211840002)

摘　　要：以合成的PEG2000-Br为引发剂,甲基丙烯酸二乙基氨基乙酯(DEAM)为功能性单体,CuBr为催化剂,五甲基二乙烯基三胺(PMDETA)为配体,通过原子转移自由基聚合(ATRP)制备了两亲聚合物聚乙二醇-聚甲基丙烯酸二乙基氨基乙酯(PEG-PDEAM);并通过紫外、1 H-NMR等表征手段对聚合物的结构进行了表征;实验以荧光染料DPH为探针,分析探讨了两亲聚合物的临界胶束浓度(CMC)值,并以PEG-PDEAM为载体,阿霉素(DOX)为模型药物,分析了聚合物对脂溶性药物的包载能力,以及载药胶团在不同介质或温度下的药物控释能力。结果表明:PEG-PDEAM对DOX的最高包封率为64.62%,载药量为8.077%;DOX-PEG-PDEAM聚合物胶团有良好的酸响应能力,12h内可实现90%药物释放;并且该聚合物胶团亦具有一定的温度响应能力,在低温条件下释放效率显著的低于高温情况下。Acid sensitive polymeric micelles have great potential as carriers for target drug delivery systems. PEGzooo-Br was synthesized. Amphiphilic polymer PEG - diethylaminoethyl methacrylate（PEG-PDEAM）with diethyl amino ethyl two methacrylic acid as functional monomer and pentamethyl diethylenetriamine （PMDETA） as a ligand, were prepared by the atom transfer radical polymerization of PEG-PDEAM using PEGzooo-Br. And by UV and 1 H-NMR polymer structures were characterized. The critical micelle concentration （CMC） of the polymer was analyzed with DPH as a probe. And PEG-PDEAM as the carrier, doxorubicin （OOX） as a model drug, the carrying capacity of the polymer for lipophilic drug, and the controlled drug delivery capabilities of drug-loaded micelles in different media or temperature were analyzed. The results showed that the encapsulation efficiency of OOX-PEG-PDEAM up to 64.62%, the drug loading 8. 077%. OOX-PEG-PDEAM micelles had good acidic response capability, 90% of the drug can be released within 12h in vitro. And the polymer micelles also had a certain temperature response capability at low temperatures significantly lower than that under high temperature conditions.

关 键 词：PEG-PDEAM 酸敏感 体外释放 DOX 

分 类 号：TQ460.1[化学工程—制药化工]