Synthesis and Characterization of Amphiphilic Glycidol-Chitosan-Deoxycholic Acid Nanoparticles as a Drug Carrier for Doxorubicin
Synthesis and Characterization of Amphiphilic Glycidol-Chitosan-Deoxycholic Acid Nanoparticles as a Drug Carrier for Doxorubicin
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DOI：
10.1021/bm100989x
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发表时间：
2010-12-01
影响因子：
6.2
通讯作者：
Ma, Xiaojun
中科院分区：
文献类型：
--
作者：
Zhou, Huofei;Yu, Weiting;Ma, Xiaojun
通过疏水部分脱氧胆酸（DCA）和亲水部分缩水甘油的接枝，合成了新型两亲性壳聚糖衍生物缩水甘油壳聚糖脱氧胆酸（G-CS-DCA），用于制备难溶性药物的载体。基于自我组装。G-CS-DCA可形成粒径在160 ~ 210 nm的纳米粒，在室温下PBS（pH7.4）中保存3个月左右仍保持稳定的结构。随着DCA取代度（DS）的增加，临界聚集浓度从0.043 mg/mL降低到0.013 mg/mL。G-CS-DCA纳米粒能够很好地包裹阿霉素（DOX），在37 ℃的PBS（pH7.4）中，DOX能够保持缓释而不突释。体外抗肿瘤实验结果表明，不同浓度的DOX-G-CS-DCA纳米粒对MCF-7细胞具有明显的抗肿瘤活性。荧光成像结果表明DOX-G-CS-DCA纳米粒可被MCF-7细胞轻易摄取。这些结果表明，G-CS-DCA纳米粒可能是一种有前途的载体，用于癌症治疗中的DOX递送。
Novel amphiphilic chitosan derivatives (glycidol chitosan deoxycholic acid, G-CS-DCA) were synthesized by grafting hydrophobic moieties, deoxycholic acid (DCA), and hydrophilic moieties, glycidol, with the purpose of preparing carriers for poorly soluble drugs. Based on self-assembly. G-CS-DCA can form nanoparticles with size ranging from 160 to 210 nm, and G-CS-DCA nanoparticles maintained stable structure for about 3 months when stored in PBS (pH 7.4) at room temperature. The critical aggregation concentration decreased from 0.043 mg/mL to 0.013 mg/mL with the increase of degree of substitution (DS) of DCA. Doxorubicin (DOX) could be easily encapsulated into G-CS-DCA nanoparticles and keep a sustained release manner without burst release when exposed to PBS (pH 7.4) at 37 degrees C. Antitumor efficacy results showed that DOX-G-CS-DCA have significant antitumor activity when MCF-7 cells were incubated with different concentration of DOX-G-CS-DCA nanoparticles. The fluorescence imaging results indicated DOX-G-CS-DCA nanoparticles could easily be uptaken by MCF-7 cells. These results suggested that G-CS-DCA nanoparticles may be a promising carrier for DOX delivery in cancer therapy.