5-氟尿嘧啶/壳聚糖载药纳米微球的制备及性能  

Preparation and character of 5-fluorouracil/chitosan drug-loaded nanospheres

作　　者：杨培慧[1] 刘媚[1] 张建莹[1] 李周明[1] 蔡继业[1] 

机构地区：[1]暨南大学化学系,广东广州510632

出　　处：《化学研究与应用》2009年第1期42-46,共5页Chemical Research and Application

基　　金：国家自然科学基金(60578025);广东省自然科学基金(021190);广州市科技计划项目基金(2003Z3-D2041)资助项目

摘　　要：以三聚磷酸钠为交联剂,采用离子交联法制备了5-氟尿嘧啶/壳聚糖纳米微球,评价其性能、体外释药性能及对人肺癌细胞GLC-82的体外杀伤效应,并通过Zeta电位和红外光谱分析载药纳米微球形成机理。结果表明,所制备的5-Fu/CS纳米微球平均包封率为32.3%,平均载药量为25.6%,平均粒径为253nm,平均Zeta电势为+8.38mV,成球性及分散性良好。CS载药纳米微球具有缓释性能,体外释药行为符合双向动力学规律。在体外作用72h,CS载药纳米微球对人肺癌细胞GLC-82的杀伤率达66.6%,杀伤效果明显优于5-Fu对照组。5-Fluorouracil （5-Fu）/Chitosan （CS）drug-loaded nanospheres is prepared by ionic crosslinking method with tripolyphosphate（TPP） as crosslinker. The combinative mechanism of 5-Fu/CS drug-loaded nanospheres is analyzed by Zeta potential and FTIR spectra. The results show that the means encapsulation rate, the means loading-drug rate, the means diameter and the means Zeta potential are 32.3%, 25.6%, 253nm, ＋ 8.38mV respectively. 5-Fu/CS drug-loaded nanospheres is spherical in shape and dispersive. The change of Zeta potential and FTIR spectra indicated that drug-loaded nanospheres are prepared by the process that CS erosslinkod with TPP by electrostatic process after integrating with 5-Fu. The experiment in vitro show that the releasing property of 5-Fu/CS drag-loaded nanospheres is consistent with the two phase kinetic law. The inhibitory rate of 5-Fu/CS drug-loaded nanospheres on GLC-82 cells in vitro 72h reached 66.6%. The execution of 5-Fu/CS drug-loaded nanospheres groups are better than that of 5-Fu groups.

关 键 词：载药纳米微球 壳聚糖 5-氟尿嘧啶 控制释放 杀伤效应 

分 类 号：O636.1[理学—高分子化学]