酸敏释药胶束肿瘤靶向给药系统的研究进展Progressinthe-药学学报.pdfVIP

440 药学学报 Acta Pharmaceutica Sinica 2012, 47 (4) : 440 445 酸敏释药胶束肿瘤靶向给药系统的研究进展 黄榕彬, 唐国涛* (南华大学药物药理研究所, 湖南 衡阳 421001) 摘要: 酸敏释药胶束作为一种新型的靶向给药系统, 具有增溶疏水性药物、载药量高, 酸敏感释药等优势。 可通过物理包埋或酸敏感键共价连接药物的方式包载药物。在肿瘤组织的偏酸环境下, 物理包埋载药胶束由于 共聚物亲脂嵌段质子化或亲水亲脂嵌段水解分离、共聚物失去两亲性, 胶束解聚释药; 而以共价连接方式包载 的药物经酸敏键断裂释放。现主要从载药方式 释药机制方面探讨酸敏释药胶束作为肿瘤靶向给药系统的研究 进展。 关键词: 胶束; 酸敏释药; 肿瘤靶向 中图分类号: R943 文献标识码:A 文章编号: 05 13-4870 (2012) 04-0440-06 Progress in the study of acid-sensitive micelles for the targeting drug delivery system * HUANG Rong-bin, TANG Guo-tao (Institute of Pharmacy Pharmacology, University of South China, Hengy ang 421001, China) Abstract: As a novel targeting drug delivery system, acid-sensitive micelles have many advantages, such as increasing solubility of lipophilic drugs, acid-sensitive release, high drug loading, etc. They can load drugs though non-covalent encapsulation and covalent conjugation methods. In tumor tissues, drugs are released quickly from the depolymerized micelles with lipophilic copolymer protonation or lypohydrophilic copolymer hydrolysis and covalent conjugated drugs are released when the acid-sensitive covalent linkage breaks. This review mainly advances acid-sensitive micelles for the tumor targeting drug delivery systems from drug-loaded methods and release mechanisms. Key words: micelle; acid-sensitive release; tumor targeting 聚合物胶束是一类由两亲性共聚物形成的胶束 有效增溶疏水性药物并使药物在人体内缓慢释放, 体系