Self-assembled nanoparticles based on chondroitin sulfate-deoxycholic acid conjugates for docetaxel delivery: Effect of degree of substitution of deoxycholic acid
Self-assembled nanoparticles based on chondroitin sulfate-deoxycholic acid conjugates for docetaxel delivery: Effect of degree of substitution of deoxycholic acid
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DOI：
10.1016/j.colsurfb.2016.06.019
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发表时间：
2016-10-01
影响因子：
5.8
通讯作者：
Zhai, Guangxi
中科院分区：
文献类型：
--
作者：
Liu, Mengrui;Du, Hongliang;Zhai, Guangxi
开发了基于硫酸软骨素的具有不同程度的脱氧胆酸（DOCA）取代（DS）的疏水改性聚合物用于多西他赛递送。以己二酰肼为连接基，通过酰胺键合成了硫酸软骨素-脱氧胆酸（CSAD）生物复合物。它们的特征在于球形，平均直径约为165.2 nm，负zeta电位（-14.87至20.53 mV）。DOCA DS的增加减小了纳米颗粒的尺寸，同时增加了载药效率。体外释药呈现三相缓释模式，随着DOCA在聚合物上的取代度增加，累积释药百分率增加。具有较高DS的自组装体也具有增强的纳米颗粒内化和在细胞水平上更强的细胞毒性。自组装纳米粒是一种优良的靶向给药系统，通过改变DS可以达到预期的治疗效果。(C)© 2016 Elsevier B. V.版权所有。
Hydrophobically-modified polymers based on chondroitin sulfate with different degree of substitution (DS) of deoxycholic acid (DOCA) were developed for docetaxel delivery. Chondroitin sulfate-deoxycholic acid (CSAD) bioconjugates were synthesized via the linker of adipic dihydrazide by amide bond. They were characterized with spherical shape, mean diameter of around 165.2 nm and negative zeta potential (-14.87 to 20.53 mV). An increase of DOCA DS reduced size of nanoparticles, while increasing drug loading efficiency. Drug release in vitro showed a triphasic sustained pattern and higher accumulative drug release percentage was observed with increased DS of DOCA on polymer. Self-assemblies with higher DS also had enhanced internalization of nanoparticles and stronger cytotoxicity at the cellular level. The self -assemble nanoparticles demonstrate to be excellent targeting drug delivery systems and the desired therapeutics can be achieved via the alteration of DS. (C) 2016 Elsevier B.V. All rights reserved.