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作为药物和基因递送纳米载体的聚合物胶束的当前状态、成就及未来前景

Current state, achievements, and future prospects of polymeric micelles as nanocarriers for drug and gene delivery.

作者信息

Nishiyama Nobuhiro, Kataoka Kazunori

机构信息

Center for Disease Biology and Integrative Medicine, Graduate School of Medicine, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.

出版信息

Pharmacol Ther. 2006 Dec;112(3):630-48. doi: 10.1016/j.pharmthera.2006.05.006. Epub 2006 Jul 11.

Abstract

Polymeric micelles, self-assemblies of block copolymers, are promising nanocarrier systems for drug and gene delivery. Until now, several micellar formulations of antitumor drugs have been intensively studied in preclinical and clinical trials, and their utility has been demonstrated. Even compared with long-circulating liposomes, polymeric micelles might have several advantages, such as controlled drug release, tissue-penetrating ability and reduced toxicity such as hand-foot syndrome and hypersensitivity reaction. Importantly, critical features of the polymeric micelles as drug carriers, including particle size, stability, and loading capacity and release kinetics of drugs, can be modulated by the structures and physicochemical properties of the constituent block copolymers. Also, nano-engineering of block copolymers might allow the preparation of polymeric micelles with integrated smart functions, such as specific-tissue targetability, as well as chemical or physical stimuli-sensitivity. Thus, polymeric micelles are nanotechnology-based carrier systems that might exert the activity of potent bioactive compounds in a site-directed manner, ensuring their effectiveness and safety in the clinical use.

摘要

聚合物胶束是嵌段共聚物的自组装体,是用于药物和基因递送的很有前景的纳米载体系统。到目前为止,几种抗肿瘤药物的胶束制剂已在临床前和临床试验中得到深入研究,其效用也已得到证实。即使与长循环脂质体相比,聚合物胶束也可能具有几个优点,如可控的药物释放、组织穿透能力以及减少诸如手足综合征和过敏反应等毒性。重要的是,作为药物载体的聚合物胶束的关键特性,包括粒径、稳定性、药物负载能力和释放动力学,可以通过组成嵌段共聚物的结构和物理化学性质来调节。此外,嵌段共聚物的纳米工程可能允许制备具有集成智能功能的聚合物胶束,如特定组织靶向性以及化学或物理刺激敏感性。因此,聚合物胶束是以纳米技术为基础的载体系统,可能以位点定向的方式发挥强效生物活性化合物的活性,确保其在临床应用中的有效性和安全性。

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