载5-氟尿嘧啶纳米球的表征

Characterization of 5-Fluorouracil Loaded Nanospheres

5-氟尿嘧啶广泛用于治疗肝癌、乳腺癌等各种肿瘤,但却严重损伤骨髓、心脏等重要器官。为降低其毒副作用,以可生物降解的α-氰基丙烯酸正丁酯为载体,采用乳液聚合技术,制备了5-氟尿嘧啶聚α-氰基丙烯酸正丁酯纳米球。扫描电镜显示纳米球呈规则球形,平均粒径(181±17)nm,有利于通过网状内皮系统的摄取和肿瘤的高渗透和截留效应,实现肝及肝部肿瘤组织的被动靶向。紫外分光光度计测得纳米球载药量为41%。体外实验显示,纳米球体外释放呈两相特征,缓释相约9 h,表明α-氰基丙烯酸正丁酯纳米球能作为5-氟尿嘧啶的缓释载体,这将推动5-氟尿嘧啶新剂型的合成与发展。

5-Fluorouracil（5-Fu）commonly used in treatment of liver cancer and breast cancer produces undesirable side effects such as damage of marrow and cardiotoxicity. To reduce the side effects, nanospheres loaded with 5-Fu was prepared by emulsion polymerization of biodegradable butyl acyanoacrylate （BCA） with 5-Fu. The nanospheres are uniform, smooth and spherical and the average size is 181±17 nm as characterized by SEM,which favors the uptake of reticuloendothelial system （RES） in liver and the enhanced permeability and retention effect （EPR） in most solid tumor for passive targeting on liver and tumor tissue of liver. The 5-Fu loading of the nanospheres is 41% as determined by UV. The release of 5-Fu from 5-Fu-loaded nanospheres in vitro follows a biphasic process with a gradual release over 9 h. It is suggested that the developed BCA nanospheres drug delivery system is suitable for sustaining carrier of 5-Fu and promotes the new 5-Fu pharmaceutical synthesis and development.