壳聚糖基多功能纳米药物载体的体外研究

制备了一种壳聚糖基多功能纳米药物载体系统, 并探讨了其体外释药性质. 合成了甲氨蝶呤-壳聚糖偶联物(MTX-CS), 甲氨喋呤(MTX)的取代度为6.3%; MTX-CS具有两亲性, 在水性介质中能自组装形成纳米粒子, 平均粒径为(269.5±18.3) nm, zeta电位为(25.7±0.9) mV. MTX-CS纳米粒子能有效包载抗血管生成药Combretastatin A-4(CA-4), 当药物/载体材料投料比为1∶4 时, 载药量为15.7%, 包封率为62.8%. 体外释放实验结果显示, CA-4释放较快, MTX释放缓慢, 有利于发挥2种药物的协同抗肿瘤作用.

In vitro Studies of Chitosan-based Multifunctional Drug Delivery Nanosystem

The preparation method of a chitosan-based multifunctional nano-drug carrier system and its drug release properties were reported. Methotrexate conjugated chitosan(MTX-CS) was synthesized and characterized, and the substitution degree of MTX was 6.3%. MTX-CS had amphiphilic property, thus could form self-assembled nanoparticles in aqueous medium. The mean diameter of MTX-CS nanoparticles was (269.5±18.3) nm, and the zeta potential was (25.7±0.9) mV. MTX-CS nanoparticles could effectively load antitumor drugcombretastatin A-4(CA-4); CA-4 loading content and entrapment efficiency were 15.7% and 62.8%, respectively, when the feed mass ratio of drug and carrier was 1∶4. The in vitro release experiment shows that CA-4 rapidly releases from MTX-CS nanoparticles, but MTX release rate obviously slows, which is favorable for the combination tumor therapy.