高等学校化学学报 ›› 2012, Vol. 33 ›› Issue (07): 1586-1590.doi: 10.3969/j.issn.0251-0790.2012.07.039

• 高分子化学 • 上一篇    下一篇

壳聚糖基多功能纳米药物载体的体外研究

陈柔, 杨金荣, 杨晓英, 王玉玫, 李蓉珊, 王润玲, 王银松   

  1. 天津市临床药物关键技术重点实验室, 天津医科大学药学院, 天津 300070
  • 收稿日期:2011-09-13 出版日期:2012-07-10 发布日期:2012-07-10
  • 通讯作者: 王银松, 女, 博士, 副教授, 主要从事生物高分子材料及其纳米药物载体研究. E-mail: wangyinsong@tijmu.edu.cn E-mail:wangyinsong@tom.com
  • 基金资助:

    国家自然科学基金(批准号: 30900303)和博士后基金(批准号: 20100480654, 201104308)资助.

In vitro Studies of Chitosan-based Multifunctional Drug Delivery Nanosystem

CHEN Rou, YANG Jin-Rong, YANG Xiao-Ying, WANG Yu-Mei, LI Rong-Shan, WANG Rui-Ling, WANG Yin-Song   

  1. Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics(Theranostics), School of Pharmacy, Tianjin Medical University, Tianjin 300070, China
  • Received:2011-09-13 Online:2012-07-10 Published:2012-07-10

摘要: 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.

关键词: 壳聚糖, 多功能纳米粒子, 甲氨喋呤, Combretastatin A-4, 肿瘤联合治疗

Abstract: 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.

Key words: Chitosan, Multifunctional nanoparticles, Methotrexate, Combretastatin A-4, Combination tumor therapy

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