半乳糖化壳聚糖—氟尿嘧啶偶合物纳米给药体系的制备、表征及体外性能研究  

Fabrication,Characterization and in Vitro Performance Evaluation of GC-FUA Based Nanoparticles Delivery System

作　　者：李娜梅[1] 杨飒[1] 宁倩[1] 黄灿[1] 黄文[1] 贺子宁 贺冬秀[1] 喻翠云[1] 

机构地区：[1]南华大学药物药理研究所,湖南衡阳421001

出　　处：《南华大学学报（自然科学版）》2015年第3期82-86,91,共6页Journal of University of South China：Science and Technology

基　　金：国家自然科学基金资助项目(81471177);湖南省科学技术厅基金资助项目(2014GK3082);南华大学抗肿瘤药物创新团队;南华大学青年英才计划

摘　　要：以预先合成的半乳糖化壳聚糖—氟尿嘧啶偶合物(GC-FUA)为原料,采用离子交联法制备出了GC-FUA纳米给药体系,并结合单因素分析法筛选出其最佳制备条件为GC-FUA浓度2.0 mg/m L,TPP浓度1.0 mg/m L,p H值4.5,GC-FUA/TPP质量比12∶1.应用SEM、UV等表征该纳米给药体系多呈球形,大小较均一,且具有缓释性能;采用MTT法观察5-Fu、物理包封5-Fu GC纳米粒子、GC-FUA纳米粒子对Hep G2细胞的增殖抑制作用.结果表明三者对Hep G2细胞的增殖具有明显抑制作用,且呈剂量依赖性,GC-FUA纳米粒子作用较5-Fu和物理包封5-Fu GC纳米粒子明显增强.In this experiment, N-galactosylated-chitosan-5-fluorouracil acetic acid conjugate （GC- FUA ） which we previously synthesized nanoparticles, were produced by ionic crosslinking method based on modified ionic gelation of tripolyphosphate （TPP） with GC- FUA. The effects of GC-FUA concerntration, TPP concerntration, pH value, etc. on the preparation of GC-FUA nanoparticles were evaluated. And results were when GC-FUA concerntration was 2.0 mg/mL, TPP concerntration was 1.0 mg/mL, pH value was 4.5, GC-FUA/TPP mass ratio was 12： 1, opalescent solution of stable GC-FUA nanoparticles could be easily obtained. GC-FUA nanoparticles exhibited regularly spherical shapes, with a smooth surface and uniform size, and has a slow release properties which were confirmed by SEM and Nano ZS. Cytotoxicity study （MTT） in HepG2 cell lines demonstrated that the resulting GC-FUA nanoparticles were more potent in killing cancer cells, compared to free 5-fluorouracil （5-Fu） and 5-Fu-loaded GC nanoparticles.

关 键 词：GC-FUA纳米给药体系 5-FU 缓释 HEPG2 

分 类 号：R94[医药卫生—药剂学]