载药聚合物胶束的临床研究进展。

Progress of drug-loaded polymeric micelles into clinical studies.

机构信息

Department of Bioengineering, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan.

Department of Bioengineering, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan; Center for Disease Biology and Integrative Medicine, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8656, Japan; Department of Materials Engineering, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-8654, Japan.

出版信息

J Control Release. 2014 Sep 28;190:465-76. doi: 10.1016/j.jconrel.2014.06.042. Epub 2014 Jun 30.

DOI:10.1016/j.jconrel.2014.06.042

PMID:24993430

Abstract

Targeting tumors with long-circulating nano-scaled carriers is a promising strategy for systemic cancer treatment. Compared with free small therapeutic agents, nanocarriers can selectively accumulate in solid tumors through the enhanced permeability and retention (EPR) effect, which is characterized by leaky blood vessels and impaired lymphatic drainage in tumor tissues, and achieve superior therapeutic efficacy, while reducing side effects. In this way, drug-loaded polymeric micelles, i.e. self-assemblies of amphiphilic block copolymers consisting of a hydrophobic core as a drug reservoir and a poly(ethylene glycol) (PEG) hydrophilic shell, have demonstrated outstanding features as tumor-targeted nanocarriers with high translational potential, and several micelle formulations are currently under clinical evaluation. This review summarizes recent efforts in the development of these polymeric micelles and their performance in human studies, as well as our recent progress in polymeric micelles for the delivery of nucleic acids and imaging.

摘要

利用长循环纳米载体靶向肿瘤是一种有前途的系统癌症治疗策略。与游离的小分子治疗剂相比，纳米载体可以通过增强的通透性和保留（EPR）效应选择性地在实体瘤中积累，EPR 效应的特征是肿瘤组织中血管渗漏和淋巴引流受损，从而实现更好的治疗效果，同时减少副作用。在这种情况下，载药聚合物胶束，即由疏水性核作为药物储库和聚（乙二醇）（PEG）亲水性壳组成的两亲嵌段共聚物的自组装，已被证明具有作为肿瘤靶向纳米载体的突出特性，具有很高的转化潜力，目前有几种胶束制剂正在进行临床评估。本综述总结了这些聚合物胶束的最新研究进展及其在人体研究中的表现，以及我们在用于核酸递药和成像的聚合物胶束方面的最新进展。