Group of Polymeric Materials for the Controlled Release of Bioactive Compounds in Biomedicine, Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense de Madrid, Spain.
J Biomed Mater Res A. 2012 Jun;100(6):1467-76. doi: 10.1002/jbm.a.34051. Epub 2012 Mar 6.
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.
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。
