Na Kun
Department of Biotechnology, The Catholic University of Korea, Bucheon, Korea.
Korean J Gastroenterol. 2007 May;49(5):314-9.
Polymeric micelles from pH-sensitive block copolymers have been designed for targeting tumor acidity or endosomal pH in tumor cells. The micelles are core-shell types formed by self-organization of the blocks in an aqueous medium or under specific experimental conditions. They possess a segment that has physical or chemical properties responding to small changes in environmental pH. The segment induces to the fast release kinetics from the micelles at tumor sites by particle shrunk/disruption. Furthermore, it can alter the biodistribution of the micelles and the interactions with tissues and cells by utilizing small pH changes. Such properties lead to overcome the problems associated with free chemo-agents, such as nonspecific toxicity, lack of tumor selectivity, and the development of multidrug resistance in various tumor cells. Therefore, the micelles have been considered as promising anti-cancer drug carriers. This review summarizes the recent progress in pH-sensitive micelles for tumor chemotherapy, particularly for those responding to tumor pH and endosomal/lysosomal pH for the treatment of multidrug resistance (MDR).
基于pH敏感型嵌段共聚物的聚合物胶束已被设计用于靶向肿瘤酸度或肿瘤细胞内体的pH值。这些胶束是核壳型的，由嵌段在水性介质中或特定实验条件下自组装形成。它们具有一个对环境pH值的微小变化具有物理或化学响应特性的片段。该片段通过粒子收缩/破坏诱导胶束在肿瘤部位实现快速释放动力学。此外，它可以利用微小的pH变化改变胶束的生物分布以及与组织和细胞的相互作用。这些特性有助于克服与游离化疗药物相关的问题，如非特异性毒性、缺乏肿瘤选择性以及各种肿瘤细胞中多药耐药性的产生。因此，胶束被认为是很有前景的抗癌药物载体。本综述总结了用于肿瘤化疗的pH敏感型胶束的最新进展，特别是那些对肿瘤pH值以及内体/溶酶体pH值有响应以治疗多药耐药性（MDR）的胶束。
