生物可降解聚酯用作蛋白质药物控释载体  

Biodegradable Polyesters and Their Derivatives for Protein Delivery

作　　者：卢婷利[1] 陈涛[1] 胡惠静[1] 

机构地区：[1]西北工业大学生命科学院,西安710072

出　　处：《高分子通报》2007年第7期55-60,共6页Polymer Bulletin

基　　金：陕西省自然基金资助项目(2006B12);中国博士后基金资助项目(20060390322)

摘　　要：聚乳酸PLA及乳酸与羟基乙酸的共聚物PLGA,由于其良好的生物相容性以及生物降解性,可用作蛋白质类药物控释体系的载体材料,同时可延长蛋白质药物的释放。本文综述了几种生物相容性聚酯及其衍生物以及它们的形成方法:(1)在PLGA的分子链中引入亲水性的含醚键的分子如PEO、PEG,来提高聚合物的亲水性,形成PLGA嵌段共聚物;(2)将细胞可接受的片段或多肽固定在聚合物支架表面,来增强PLGA与细胞间的粘附力,得到靶向的PLGA衍生物;(3)改变PLGA载体内的酸性环境,提高蛋白质药物在载体中的稳定性,发展了支化聚酯PVA-g-PLGA,并得到均速的药物释放。以上这些方法所得到的聚酯及其衍生物,均可作为蛋白质类药物安全、可靠的载体材料。Biodegradable polyesters, such as PLA and PLGA, have proven to be very useful protein delivery sustained release vehicle material and can provide prolonged protein release thanks to their good biocompatibility and biodegradability. This review provides an applicable summary of different formulation routes to forming polyesters and their derivatives for the purpose of （ 1 ） improving the hydrophilic property of PLGA through introducing molecule having ether bond, such as PEO, PEG, in PLGA and forming PLGA block copolymer; （2） enhancing the adhesion of vehicle and cell by immobilizing the cell-recognizable ligand moiety and/or peptide onto the surface of biodegradable polymer scaffolds and achieving targeted PLGA derivatives; and （3） developing novel branched polyesters PVA-g- PLGA and obtaining zero-order drug release kinetics through changing the acid microclimate in PLGA vehicle and improving the stability of protein inner the vehicle. All of the above PLGA and their derivatives can produce safe, qualified and efficacious vehicle for protein and peptide drug delivery system.

关 键 词：生物降解聚酯 线性PLGA 靶向PLGA 支化PVA—g—PLGA 

分 类 号：TQ460.4[化学工程—制药化工]