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载多西紫杉醇金纳米粒子的合成及体外研究。

Synthesis and in vitro studies of gold nanoparticles loaded with docetaxel.

机构信息

Universidade do Estado do Rio de Janeiro, Instituto de Química, Brazil.

出版信息

Int J Pharm. 2013 Oct 1;454(2):703-11. doi: 10.1016/j.ijpharm.2013.05.031. Epub 2013 May 21.

Abstract

The aim of these studies was to synthesize, characterize and evaluate the efficacy of pegylated gold nanoparticles (AuNPs) that differed in their PEG molecular weight, using PEG 550 and PEG 2000. The synthesis of the gold nanoparticles was carried out by modified Brust method with a diameter of 4-15 nm. The targeting agent folic acid was introduced by the covalent linkage. Finally, the anti-cancer drug docetaxel was encapsulated by the AuNPs by non covalent adsorption. The nanoparticles were characterized by transmission electron microscopy and used for in vitro studies against a hormone-responsive prostate cancer cell line, LnCaP. The loaded nanoparticles reduced the cell viability in more than 50% at concentrations of 6 nM and above after 144 h of treatment. Moreover, observation of prostate cancer cells by optical microscopy showed damage to the cells after exposure to drug-loaded AuNPs while unloaded AuNPs had much less effect.

摘要

这些研究的目的是合成、表征和评估聚乙二醇化金纳米粒子(AuNPs)的功效,这些纳米粒子的聚乙二醇分子量不同,使用了聚乙二醇 550 和聚乙二醇 2000。金纳米粒子的合成采用了改良的 Brust 方法,直径为 4-15nm。靶向剂叶酸通过共价键连接引入。最后,通过非共价吸附将抗癌药物多西紫杉醇包封在 AuNPs 中。通过透射电子显微镜对纳米粒子进行了表征,并用于针对激素反应性前列腺癌细胞系 LnCaP 的体外研究。负载纳米粒子的浓度在 6 nM 及以上时,在 144 h 的治疗后,细胞活力降低了 50%以上。此外,光学显微镜观察前列腺癌细胞显示,暴露于载药 AuNPs 后细胞受损,而未载药 AuNPs 的影响要小得多。

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