Shandong University, School of Pharmaceutical Science, Department of Pharmaceutics, Ji'nan, PR China.
Expert Opin Drug Deliv. 2012 Jul;9(7):805-22. doi: 10.1517/17425247.2012.689284. Epub 2012 May 19.
During the past decades, polymer-drug conjugates are one of the hottest topics in novel drug development fields. Amphiphilic polymer-drug conjugates in aqueous solution could form micelles or micelle-like nanoassemblies. Compared with polymer-drug conjugates and the micelles into which drugs are physically entrapped, micelles or micelle-like nanoassemblies based on polymer-drug conjugates bring several additional advantages, including increased drug-loading capacity, enhanced intracellular uptake, reduced systemic toxicity, and improved therapeutic efficacy.
This review focuses on recent progress achieved in the research field of micelles or micelle-like nanoassemblies based on polymer-drug conjugates. Firstly, properties of polymers, drugs, and linkers which could be used to build polymer-drug conjugate micelles or micelle-like nanoassemblies are summarized. Then, the characterization methods are described. Finally, the drug-targeting mechanisms are discussed. Micelles or micelle-like nanoassemblies based on polymer-drug conjugates as an emerging platform have the potential to achieve medical treatments with enhanced therapeutic effect.
The application of micelles or micelle-like nanoassemblies based on polymer-drug conjugates may give new life to old active compounds abandoned due to their low solubility problems. For clinical application, there is a need to further optimize the properties of the polymer, drug, and linker.
在过去几十年中,聚合物-药物偶联物是新型药物开发领域中最热门的话题之一。两亲性聚合物-药物偶联物在水溶液中可以形成胶束或胶束样纳米组装体。与药物物理包埋的聚合物-药物偶联物和胶束相比,基于聚合物-药物偶联物的胶束或胶束样纳米组装体具有几个额外的优势,包括增加载药量、增强细胞内摄取、降低系统毒性和提高治疗效果。
本文重点介绍了基于聚合物-药物偶联物的胶束或胶束样纳米组装体研究领域的最新进展。首先,总结了可用于构建聚合物-药物偶联物胶束或胶束样纳米组装体的聚合物、药物和连接子的性质。然后,描述了表征方法。最后,讨论了药物靶向机制。基于聚合物-药物偶联物的胶束或胶束样纳米组装体作为一种新兴平台,有可能实现具有增强治疗效果的医疗治疗。
基于聚合物-药物偶联物的胶束或胶束样纳米组装体的应用可能会为由于溶解度问题而被废弃的老的活性化合物带来新的生命。对于临床应用,需要进一步优化聚合物、药物和连接子的性质。