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来自水溶性聚合物脂质衍生物的胶束作为难溶性药物的递送系统。

Micelles from lipid derivatives of water-soluble polymers as delivery systems for poorly soluble drugs.

作者信息

Lukyanov Anatoly N, Torchilin Vladimir P

机构信息

Department of Pharmaceutical Sciences, School of Pharmacy, Bouve College of Health Sciences, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.

出版信息

Adv Drug Deliv Rev. 2004 May 7;56(9):1273-89. doi: 10.1016/j.addr.2003.12.004.

Abstract

Polymeric micelles have a whole set of unique characteristics, which make them very promising drug carriers, in particular, for poorly soluble drugs. Our review article focuses on micelles prepared from conjugates of water-soluble polymers, such as polyethylene glycol (PEG) or polyvinyl pyrrolidone (PVP), with phospholipids or long-chain fatty acids. The preparation of micelles from certain polymer-lipid conjugates and the loading of these micelles with various poorly soluble anticancer agents are discussed. The data on the characterization of micellar preparations in terms of their morphology, stability, longevity in circulation, and ability to spontaneously accumulate in experimental tumors via the enhanced permeability and retention (EPR) effect are presented. The review also considers the preparation of targeted immunomicelles with specific antibodies attached to their surface. Available in vivo results on the efficiency of anticancer drugs incorporated into plain micelles and immunomicelles in animal models are also discussed.

摘要

聚合物胶束具有一系列独特的特性,这使其成为非常有前景的药物载体,尤其是对于难溶性药物而言。我们的综述文章聚焦于由水溶性聚合物(如聚乙二醇(PEG)或聚乙烯吡咯烷酮(PVP))与磷脂或长链脂肪酸的共轭物制备的胶束。讨论了由某些聚合物 - 脂质共轭物制备胶束以及用各种难溶性抗癌剂负载这些胶束的方法。呈现了关于胶束制剂在形态、稳定性、循环寿命以及通过增强渗透和滞留(EPR)效应在实验性肿瘤中自发积累能力方面的表征数据。该综述还考虑了表面附着有特异性抗体的靶向免疫胶束的制备。此外,还讨论了在动物模型中普通胶束和免疫胶束中掺入的抗癌药物的体内有效性结果。

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