摘要
以不同分子量的甲氧基聚乙二醇(mPEG)和一氯乙酸为原料,通过酯化反应得到氯乙酸甲氧基聚乙二醇酯,将氯乙酸甲氧基聚乙二醇酯与抗肿瘤药物5-氟尿嘧啶(5-FU)结合制备了不同分子量的mPEG-5-FU前药并进行了红外、核磁和紫外的表征。结果表明,5-FU已经成功接到了聚乙二醇链的末端。随着mPEG分子量的提高,前药的水溶性增强。当mPEG的分子量为2000时,mPEG_(2000)-5-FU的载药量为9.6%,前药的水溶性最大,此时的释药率达到最大值。水解实验表明,mPEG-5-FU前药具有长效缓释的功能,它可以在不同pH值溶液中释放出5-FU或其衍生物。
A series of novel methoxypolyethylene glycol derivates was synthesized by esterification of methoxypolyethylene glycol and chloroacetic acid.Then react with 5-fluorouracil, thus the prodrugs was obtained.The mPEG-5-FU prodrugs were characterized by IR,~1H-NMR and UV spectroscopy.The result showed that 5-FU was successfully connected to the ends of mPEG through ester bond.As the molecular weight of mPEG increased, the water solubility of prodrugs improved.When the molecular weight of mPEG reached 2000,the prodrug had the best water solubility and the highest drug release rate.Drug content of mPEG_(2000)-5-FU prodrug achieved 9.6%.The hydrolysis measurement showed that the polymeric prodrugs had the function of longer duration of activity, due to slow release.The prodrugs obtained could release 5-FU or its unit in different pH solution.
作者
常军
靳梦月
王斌
胡雨虹
曹晓蝶
刘岩
郑文洁
CHANG Jun;JIN Meng-yue;WANG Bin;HU Yu-hong;CAO Xiao-die;LIU Yan;ZHENG Wen-jie(Department of Polymer Materials&Engineering,Shenyang Ligong University,Shenyang110159,China)
出处
《精细与专用化学品》
CAS
2022年第12期45-49,共5页
Fine and Specialty Chemicals
基金
辽宁省教育厅高等学校基本科研项目(LJKZ0249)
国家级大学生创新创业项目(202110144017)。
