脂质体面临的聚乙二醇“窘境”及其解决方法  

“PEG dilemma” for liposomes and its solving approaches

作　　者：张迪[1] 徐缓[1] 胡美娜[1] 邓意辉[2] 

机构地区：[1]辽宁师范大学化学化工学院,辽宁大连116029 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《药学学报》2015年第3期252-260,共9页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81102394);中国博士后科学基金资助项目(2013M530899)

摘　　要：聚乙二醇(polyethylene glycol,PEG)因其优越的性能被广泛应用于脂质体等纳米载体表面修饰,但随着研究的深入,PEG化脂质体也产生了相应的负面影响,如PEG链抑制靶细胞对脂质体的摄取、妨碍p H敏感脂质体细胞内的"核内体逃逸"以及对同一动物体内重复注射PEG化脂质体诱发的加速血液清除(accelerated blood clearance,ABC)现象等,这些称为PEG"窘境"(PEG dilemma)。PEG"窘境"为携载抗肿瘤药物的PEG化脂质体的靶向递送、包封基因和蛋白类药物的PEG化p H敏感脂质体发生有效的细胞内释放以及需要重复注射的PEG化脂质体都带来了严峻的挑战,因此解决PEG"窘境"刻不容缓。本文对PEG"窘境"的定义、分类和几种克服PEG"窘境"的方法进行了综述。Polyethylene glycol （PEG） is extensively used to increasing the in vivo and in vitro stability of liposomes. However, PEGylated liposomes also produce some negative effects with further research, such as low cellular uptake, poor “endosomal escape” of pH sensitive liposome （PSL） and accelerated blood clearance （ABC） phenomenon, and this situation is referred as the “PEG dilemma”. “PEG dilemma” posed severe challenges for the targeted delivery of PEGylated liposomes-loaded anticancer drugs, effective intracellular release of PEGylated PSL-encapsulated gene and protein drugs, and repeated administration of PEGylated liposomes. Therefore, it is urgent to solve the “PEG dilemma”. This review focused on the definition, classification of “PEG dilemma”, and discussed several possible approaches to overcome “PEG dilemma”.

关 键 词：聚乙二醇 脂质体 核内体逃逸 加速血液清除 

分 类 号：R943.4[医药卫生—药剂学]