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载阿霉素人血清白蛋白(HSA)纳米粒的制备、表征及药物疗效维持

Preparation, characterisation and maintenance of drug efficacy of doxorubicin-loaded human serum albumin (HSA) nanoparticles.

作者信息

Dreis S, Rothweiler F, Michaelis M, Cinatl J, Kreuter J, Langer K

机构信息

Institute of Pharmaceutical Technology, Biocenter Niederursel, Johann Wolfgang Goethe-University, Max-von-Laue-Strasse 9, D-60438 Frankfurt/Main, Germany.

出版信息

Int J Pharm. 2007 Aug 16;341(1-2):207-14. doi: 10.1016/j.ijpharm.2007.03.036. Epub 2007 Mar 30.

Abstract

Human serum albumin (HSA) nanoparticles represent promising drug carrier systems. Binding of cytostatics to HSA nanoparticles may diminish their toxicity, optimise their body distribution and/or may overcome multidrug resistance. In the present study, doxorubicin-loaded HSA nanoparticle preparations were prepared. Doxorubicin was loaded to the HSA nanoparticles either by adsorption to the nanoparticles' surfaces or by incorporation into the particle matrix. Both loading strategies resulted in HSA nanoparticles of a size range between 150nm and 500nm with a loading efficiency of 70-95%. The influence on cell viability of the resulting nanoparticles was investigated in two different neuroblastoma cell lines. The anti-cancer effects of the drug-loaded nanoparticles were increased in comparison to doxorubicin solution. Based on these result a standard protocol for the preparation of doxorubicin-loaded HSA nanoparticles for further antitumoural studies was established.

摘要

人血清白蛋白(HSA)纳米颗粒是很有前景的药物载体系统。细胞抑制剂与人血清白蛋白纳米颗粒的结合可能会降低其毒性,优化其体内分布和/或克服多药耐药性。在本研究中,制备了载有多柔比星的人血清白蛋白纳米颗粒制剂。多柔比星通过吸附到纳米颗粒表面或掺入颗粒基质中加载到人血清白蛋白纳米颗粒上。两种加载策略均产生了尺寸范围在150nm至500nm之间、加载效率为70 - 95%的人血清白蛋白纳米颗粒。在两种不同的神经母细胞瘤细胞系中研究了所得纳米颗粒对细胞活力的影响。与多柔比星溶液相比,载药纳米颗粒的抗癌效果有所增强。基于这些结果,建立了用于进一步抗肿瘤研究的载有多柔比星的人血清白蛋白纳米颗粒制备标准方案。

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