聚合物胶束用于铂类抗癌药物的靶向肿瘤治疗。

Polymeric micelles for targeted tumor therapy of platinum anticancer drugs.

机构信息

a Innovation Center of NanoMedicine , Kawasaki Institute of Industrial Promotion , Kawasaki , Japan.

b Department of Bioengineering , Graduate School of Engineering, The University of Tokyo , Tokyo , Japan.

出版信息

Expert Opin Drug Deliv. 2017 Dec;14(12):1423-1438. doi: 10.1080/17425247.2017.1307338. Epub 2017 Mar 23.

Abstract

Platinum anticancer drugs are effective against a wide range of tumors, though their severe adverse effects and resistance remain unresolved. A breakthrough in these drawbacks could be achieved by using polymeric micelles, i.e. nanoassemblies having a drug loaded core and a protective hydrophilic shell, incorporating platinum drugs for tumor-targeted delivery. Areas covered: The development of cisplatin- (NC-6004) and DACHPt-loaded micelles (NC-4016) has been reviewed, particularly, from the viewpoint of the effect of their structural features on the tumor-targeting efficacy. We have also described new approaches for molecular targeting by installing ligand moieties on the surface of micelles. Moreover, small platinum drugs and platinum drug-loaded nanocarriers are introduced to explain the context for developing platinum drug-loaded polymeric micelles. Expert opinion: NC-6004 and NC-4016 micelles meet critical structural and functional requirements for achieving safe and effective tumor targeting, enhancing efficacy even against drug resistant cancer cells, and have been translated into human studies, aiming to be the first-of-their-kind in the clinic. Due to their flexible design, polymeric micelles could readily integrate new features based on the knowledge arising from the human clinical trials toward the development of innovative formulations with superior performance.

摘要

铂类抗癌药物对广泛的肿瘤有效,但它们的严重不良反应和耐药性仍未得到解决。通过使用聚合物胶束(即载药内核和保护性亲水壳的纳米组装体)来实现这些缺陷的突破,可将铂类药物用于肿瘤靶向递药。

涵盖领域

本文综述了顺铂(NC-6004)和 DACHPt 载药胶束(NC-4016)的开发,特别是从其结构特征对肿瘤靶向疗效的影响的角度进行了综述。我们还描述了通过在胶束表面安装配体部分进行分子靶向的新方法。此外,还介绍了小分子铂类药物和载铂纳米载体,以说明开发载铂聚合物胶束的背景。

专家意见

NC-6004 和 NC-4016 胶束满足实现安全有效肿瘤靶向的关键结构和功能要求,提高疗效,甚至针对耐药癌细胞,已转化为人体研究,旨在成为临床首创。由于其设计灵活,聚合物胶束可以根据人体临床试验产生的知识,很容易整合新的特征,从而开发出具有卓越性能的创新制剂。

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