麦胚凝集素修饰的EGCG-明胶-壳聚糖纳米粒的制备、表征及体外抗肿瘤活性研究

发布时间：2018-01-26 10:41

  本文关键词： EGCG 壳聚糖 明胶 纳米粒 麦胚凝集素 抗肿瘤　出处：《南京中医药大学学报》2017年01期 　论文类型：期刊论文

【摘要】：目的制备麦胚凝集素(WGA)修饰的表没食子儿茶素没食子酸酯(EGCG)-明胶(Gel)-壳聚糖(Cs)纳米粒,研究其对结肠癌HT-29细胞的作用。方法以明胶及壳聚糖为载体辅料,采用静电自组装的方法制备EGCG-Gel-Cs纳米粒,以包封率为指标,通过Box-Behnken设计-效应面法(BBD-RSM)优化纳米粒的制备处方及工艺,再将经戊二醛活化的WGA修饰到纳米粒表面。采用差示扫描量热分析药物在纳米粒中的存在状态,采用细胞毒性及细胞凋亡实验,比较研究纳米粒与原料药的体外抗肿瘤活性。结果 EGCG-Gel-Cs纳米粒的最优处方:Gel与Cs的质量比为4.2,Gel与EGCG的质量比为2.82,反应温度为34℃,包封率为(74.42±0.074)%。EGCG-Gel-Cs纳米粒粒径为(264.13±6.48)nm,经过修饰后纳米粒粒径为(389.70±9.00)nm。WGA-EGCG-Gel-Cs纳米粒对HT-29细胞的细胞毒性和细胞凋亡率显著高于EGCG原料药。结论 WGA-EGCG-Gel-Cs纳米粒可显著提高细胞毒性作用。
[Abstract]:Objective to prepare the epigallocatechin gallate (EGCG) -gelatin Gelin-chitosan (CS) nanoparticles modified by wheat germ agglutinin (WGA). Methods EGCG-Gel-Cs nanoparticles were prepared by electrostatic self-assembly with gelatin and chitosan as the carrier excipients. The encapsulation efficiency was taken as the index. The preparation of nanoparticles was optimized by Box-Behnken design-effect surface method (BBD-RSM). Then the WGA activated by glutaraldehyde was modified to the surface of nanoparticles. The presence of drugs in nanoparticles was analyzed by differential scanning calorimetry (DSC). Cytotoxicity and apoptosis were tested. The in vitro antitumor activity of EGCG-Gel-Cs nanoparticles was compared with that of raw materials. Results the mass ratio of EGCG-Gel-Cs nanoparticles to CS was 4. 2. The mass ratio of Gel to EGCG is 2.82 and the reaction temperature is 34 鈩，

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