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载他莫昔芬的巯基化海藻酸钠-白蛋白纳米粒作为抗肿瘤药物传递系统。

Tamoxifen-loaded thiolated alginate-albumin nanoparticles as antitumoral drug delivery systems.

机构信息

Group of Polymeric Materials for the Controlled Release of Bioactive Compounds in Biomedicine, Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense de Madrid, Spain.

出版信息

J Biomed Mater Res A. 2012 Jun;100(6):1467-76. doi: 10.1002/jbm.a.34051. Epub 2012 Mar 6.

Abstract

Nanoparticles based on disulfide bond reduced bovine serum albumin and thiolated alginate (alginate-cysteine conjugate) have been prepared by coacervation method and have been loaded with tamoxifen (TMX). The TMX load into the nanoparticles was optimized (4-6 μg/mg NP) by freeze-drying the systems before the loading procedure. Maximum TMX release (45-52%) took place between 2 and 25 h. Cytotoxicity of unloaded nanoparticles in MCF-7 and HeLa cells was not observed, although a small decrease in viability took place at very high concentration. Cell uptake of nanoparticles occurred in both cell types and the presence of polysaccharide in the nanoparticle composition allowed a better interaction with cells. The administration of 10 μM TMX by TMX-nanoparticles was effective in both cellular lines, and the effect of the drug-loaded systems on MCF-7 cell cycle showed the efficacy of the TMX-loaded nanoparticles.

摘要

基于二硫键还原牛血清白蛋白和巯基化海藻酸盐(海藻酸钠-半胱氨酸缀合物)的纳米粒子已通过凝聚方法制备,并负载了他莫昔芬(TMX)。通过在加载程序之前冷冻干燥系统,将 TMX 负载优化至(4-6μg/mgNP)。在 2 至 25 小时之间,TMX 释放量达到最大值(45-52%)。未负载的纳米粒子在 MCF-7 和 HeLa 细胞中没有表现出细胞毒性,尽管在非常高的浓度下细胞活力略有下降。两种细胞类型都发生了纳米粒子的细胞摄取,并且纳米粒子组成中的多糖的存在允许与细胞更好地相互作用。通过 TMX-纳米粒子给予 10μM TMX 在两种细胞系中均有效,并且负载药物系统对 MCF-7 细胞周期的影响表明了负载 TMX 的纳米粒子的功效。

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