National Institute of Health Sciences, 1-18-1 Kamiyoga, Setagaya-ku, Tokyo 158-8501, Japan.
Polymer Chemistry Division, Chemical Resources Laboratory, Tokyo Institute of Technology, R1-11, 4259 Nagatsuda, Midori, Yokohama 226-8503, Japan.
J Control Release. 2015 Jul 28;210:76-83. doi: 10.1016/j.jconrel.2015.05.259. Epub 2015 May 13.
Block copolymer micelles are nanoparticles formed from block copolymers that comprise a hydrophilic polymer such as poly(ethylene glycol) and a poorly soluble polymer such as poly(amino acids). The design of block copolymer micelles is intended to regulate the in vivo pharmacokinetics, stability, and distribution profiles of an entrapped or block copolymer-linked active substance. Several block copolymer micelle products are currently undergoing clinical development; however, a major challenge in the development and evaluation of such products is identification of the physicochemical properties that affect the properties of the drug product in vivo. Here we review the overall in vitro and in vivo characteristics of block copolymer micelle products with a focus on the products currently under clinical investigation. We present examples of methods suitable for the evaluation of the physicochemical properties, non-clinical pharmacokinetics, and safety of block copolymer micelle products.
嵌段共聚物胶束是由嵌段共聚物形成的纳米颗粒，嵌段共聚物由亲水性聚合物如聚乙二醇和疏水性聚合物如聚氨基酸组成。嵌段共聚物胶束的设计旨在调节包封或嵌段共聚物连接的活性物质的体内药代动力学、稳定性和分布特征。目前有几种嵌段共聚物胶束产品正在进行临床开发；然而，在这些产品的开发和评估中面临的一个主要挑战是确定影响体内药物产品性质的理化性质。在这里，我们综述了嵌段共聚物胶束产品的整体体外和体内特征，重点介绍了目前正在临床研究的产品。我们提出了适合评估嵌段共聚物胶束产品的理化性质、非临床药代动力学和安全性的方法示例。
