5-氟尿嘧啶/明胶的制备及释药性能

Preparation and in Vitro Drug release Properties of 5-Fluorouracil/gelatin Nanocomposite

以A型明胶为原料、5-氟尿嘧啶为模型药物、异丙醇为凝聚剂,采用单凝聚法制备了5-氟尿嘧啶/明胶纳米载药颗粒（5-FU/GNPs）,并测定了纳米颗粒的粒径分布、载药量、体外缓释效果和抗肿瘤性能。结果表明：5-FU/GNPs表面形态良好,分散均一,平均粒径为（75.1±2.1）nm,载药量为23.5%±1.9%;5-FU/GNPs具有良好的缓释性能,Higuchi方程对微球的体外药物释放情况拟合度较高。四甲基偶氮唑蓝实验表明：5-FU/GNPs对胃癌细胞（SGC7901）的抑制率可达71%。

5-Fluorouracil/gelatin nanoparticles（5-FU/GNPs） were prepared by simple coacervation method using type A gelatin as raw material,5-fluorouracil as entrapped pharmaceutical,isopropanol as coacervation reagent. The particle size distribution,drug loading,in vitro drug release and antitumor activities of 5-FU/GNPs were investigated. The results showed that 5-FU/GNPs had excellent surface morphology,and dispersed uniformly with an average particle size of（75.1±2.1） nm. The average drug loading was about 23.5%±1.9%. In vitro release experiments displayed that 5-FU/GNPs exhibited good release performance,the release of 5-fluorouracil from 5-FU/GNPs accorded with the Higuchi equation,indicating that the gelatin could sustain the release of 5-fluorouracil. MTT measurement showed that 5-FU/GNPs had significant cytotoxicity on human gastric cancer cells（SGC7901）. Thus,the prepared 5-FU/GNPs could be used as a kind of drug-loading carrier in pharmaceutical field.