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

作　　者：李婷婷[1] 王振军[2] 赵乐乐[1] 郑子良 张瑞平[2] LI Ting-ting;WANG Zhen-jun;ZHAO Le-le;ZHENG Zi-liang;ZHANG Rui-ping(College of Pharmacy, Shanxi Medical University, Taiyuan 030001, Shanxi, China;Department of Image, The First Hospital of Shanxi Medical University, Taiyuan 030001, Shanxi, China;Translational Medicine Research Center, Shanxi Medical University, Taiyuan 030001, Shanxi, China)

机构地区：[1]山西医科大学药学院,山西太原030001 [2]山西医科大学第一医院影像科,山西太原030001 [3]山西医科大学转化医学研究中心,山西太原030001

出　　处：《精细化工》2018年第6期1037-1040,1067,共5页Fine Chemicals

基　　金：国家自然科学基金(81371628);山西省青年科技研究基金(201601D202105);山西医科大学校博士启动基金(03201531);山西医科大学青年基金(02201618)~~

摘　　要：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.

关 键 词：5-氟尿嘧啶 明胶 纳米颗粒 体外缓释 医药原料 

分 类 号：O636.9[理学—高分子化学]