难溶性抗肿瘤药物载体——嵌段共聚物胶束

Block copolymer micelles as delivery system for poorly soluble antineoplastic carrier

根据国外有关文献,综述了10年来嵌段共聚物胶束作为难溶性抗肿瘤药物载体的研究进展,包括嵌段共聚物胶束组成、制备方法及影响因素、理化性质和靶向特性的研究。嵌段共聚物胶束是由两亲性嵌段共聚物在水溶液中自发形成的一种自组装结构,亲水性片段形成外壳,疏水性片段形成内核,构成独特的核-壳结构。具有粒径小和粒度分布窄、载药量高和独特的体内分布等特点,可对难溶性抗肿瘤药物有效增溶、降低不良反应、提高生物利用度,不仅可以实现被动靶向给药,还可以连接具有特异性识别功能的配基对其表面进行修饰,从而实现主动靶向给药,是广阔发展前景的载药系统。

To review the research of block copolymer micelles as delivery system for poorly soluble antineoplastic carrier over the last 10 years, including the composition, preparation methods and factors which influence the loading efficiency, physicochemical properties, and targeting characteristics of block copolymer mieelles. Block copolymer micelles are self-assembled structures formed from amphiphilic block copolymers by dispersing in aqueous media. The hydrophilic blocks of the copolymer form the outer shell of the micelle, while the hydrophobic blocks form the inner core, and the proper core-shell micellar architecture was constituted. Block copolymer micelles have a whole set of unique properties, such as small sizes, narrow particle size distribution, high drug loading capacities, and available disposition characteristics in the body. Block copolymer micelles have been found as promising drug carriers due to making poorly soluble antineoplastic lysis, toxicities and side effects decrease, bioavailability increase, and targeting the drugs to specific sites in a passive way or attaching ligands in an active way, which can be specifically recognized bv receptors onto the surface of copolvmers.