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通过黏附性 4-CBS-壳聚糖/聚乳酸纳米粒增强抗拓扑异构酶 II 活性。

Enhanced anti-topoisomerase II activity by mucoadhesive 4-CBS-chitosan/poly (lactic acid) nanoparticles.

机构信息

Program of Petrochemistry and Polymer Science, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.

出版信息

Carbohydr Polym. 2013 Nov 6;98(2):1335-42. doi: 10.1016/j.carbpol.2013.08.006. Epub 2013 Aug 7.

Abstract

In this study, the biodegradable mucoadhesive 4-carboxybenzensulfonamide chitosan (4-CBS-chitosan)/poly (lactic acid) (PLA) nanoparticles were fabricated by the electrospray ionization technique for enhancing anti-topoisomerase II (Topo II) activity. The obtained (4-CBS-chitosan/PLA)-DOX nanoparticles were characterized using SEM, particle size analyzer. We emphasis on encapsulation efficiency, in vitro drug release behavior and also performed in vitro studies of Topo II inhibitory activity using gel electrophoresis. In addition, the cytotoxicity of the 4-CBS-chitosan/PLA nanoparticles using MTT assay was also studied. The mean particle size of spherical shaped (4-CBS-chitosan/PLA)-DOX is less than 300 nm. The DOX loaded 4-CBS-chitosan/PLA composite nanoparticles produced high entrapment efficiency of 85.8% and provided the prolonged release of DOX extended to 26 days and also still had strong Topo II inhibitory activity up to 77.4%. Overall, it was shown that 4-CBS-chitosan/PLA nanoparticles could be promising carriers for controlled delivery of anticancer drugs.

摘要

在这项研究中,通过电喷射电离技术制备了可生物降解的粘弹性 4-羧基苯磺酰胺壳聚糖(4-CBS-壳聚糖)/聚乳酸(PLA)纳米粒子,以增强抗拓扑异构酶 II(Topo II)活性。采用 SEM、粒度分析仪对所得(4-CBS-壳聚糖/PLA)-DOX 纳米粒子进行了表征。我们重点研究了包封效率、体外药物释放行为,并通过凝胶电泳进行了体外 Topo II 抑制活性研究。此外,还通过 MTT 测定研究了 4-CBS-壳聚糖/PLA 纳米粒子的细胞毒性。球形(4-CBS-壳聚糖/PLA)-DOX 的平均粒径小于 300nm。载有 DOX 的 4-CBS-壳聚糖/PLA 复合纳米粒子的包封效率高达 85.8%,并提供了长达 26 天的 DOX 延长释放,并且仍然具有高达 77.4%的强 Topo II 抑制活性。总体而言,结果表明 4-CBS-壳聚糖/PLA 纳米粒子可能是一种有前途的抗癌药物控释载体。

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