壳聚糖基多功能纳米药物载体的体外研究

In vitro Studies of Chitosan-based Multifunctional Drug Delivery Nanosystem

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.

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 drug-combretastatin 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.