含5-氟尿嘧啶水凝胶的制备及体外透皮释放  

Synthesis of Hydrogels Loaded 5-Fluorouracil and in vitro Evaluation for Transdermal Delivery

作　　者：刘继英[1] 张桥[1] 刘芝兰[1] 卓仁禧[1] 

机构地区：[1]武汉大学化学与分子科学学院/生物医用高分子材料教育部重点实验室,湖北武汉430072

出　　处：《武汉大学学报（理学版）》2006年第6期695-698,共4页Journal of Wuhan University:Natural Science Edition

基　　金：国家自然科学基金(20174029);国家重点基础发展规划资助项目(2005CB623903)

摘　　要：制备了一种魔芋葡甘聚糖接枝丙烯酸水凝胶,并将其作为亲水药物5-氟尿嘧啶(5-FU)透皮释放制剂基材.考察了不同魔芋葡甘聚糖与丙烯酸摩尔比的凝胶在pH 7.4的溶胀率,结果表明凝胶的溶胀率随丙烯酸含量的增加而增大.采用浸泡吸附法得到含5-FU的载药凝胶,利用改进Franz扩散池进行了离体小鼠皮肤透皮释放实验,在魔芋葡甘聚糖和丙烯酸摩尔比为1∶60,载药量为3%时获得的最大累积释放量为4 721.2μg/cm2,渗透速率为(542.2±53.0)μg.cm-2.h-1.In this paper, hydrogels of konjac glucomannan （KGM） grafted acrylic acid.（AA） were prepared for transdermal delivery matrix of hydrophilic drug 5-fluorouracil （5-FU）. The equilibrium swelling ratios （RE） of gels with different compositions were determined under environmental pH 7.4 through rat skin. It is found that the RE depends on the molar content of AA in the hydrogels. The gels loaded 5-FU was obtained by immersion dry gel into the drug solution. The penetration in vitro through rat skin of 5-FU was investigated using a modified Franz diffusion cell. The results show that, at pH 7.4 and with 3% drug loading, the maximal cumulative permeation amount 4 721.2μg/cm^2 and skin flux of （542.2±53. 0）μg·cm^-2·h^-1 can be achieved by the hydrogel with 1：60 molar ratio of KGM to AA.

关 键 词：魔芋葡甘聚糖 聚丙烯酸 水凝胶 5-氟尿嘧啶 透皮给药 

分 类 号：O633[理学—高分子化学]