PEG化聚酰胺-胺树状大分子的合成及其作为喜树碱药物载体的研究  

Synthesis of PEGylated PAMAM dendrimer as a camptothecin carrier

作　　者：戴华胄[1] 马丽芳[1] 郭丽[2] 贺世超[1] 曾国城[1] 

机构地区：[1]四川大学化学工程学院,四川成都610065 [2]四川大学华西药学院,四川成都610064

出　　处：《华西药学杂志》2009年第2期115-117,共3页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:20472055)

摘　　要：目的合成聚乙二醇(PEG)化3.0代聚酰胺-胺(PAMAM)树状大分子,并研究PEG-3.0PAMAM作为喜树碱载体的传递系统对喜树碱的溶解、释放性能和光敏性等方面的影响。方法合成PEG350-3.0PAMAM树状大分子并确证结构;用HPLC检测3.0代PAMAM及PEG350-3.0PAMAM对喜树碱溶解性能的影响;分别将3.0代PAMAM和PEG350-3.0PAMAM与喜树碱复合,检测二者对喜树碱体外释放的影响;通过光照实验考查PEG350-3.0PAMAM对喜树碱的光敏作用。结果PEG350-3.0PAMAM较之同代PAMAM对喜树碱具有更强的增溶作用和更快的释药速度,同时可改善喜树碱的光敏性,增加其稳定性。结论PEG350-3.0PAMAM作为喜树碱载体是一种很有潜力的新型药物传递系统。OBJECTIVE To synthesize PEGylated G 3.0 PAMAM and study its influence on the solubility, release and photosensitivity of CPT. METHODS PEG 350 - 3.0 PAMAM was synthesized and its structure was characterized. HPLC was employed to test the influence of G 3.0 PAMAM and PEG 350 - 3.0 PAMAM on the solubility of camptothecin（CPT）. The in vitro release of CPT after complexation with G 3.0 PAMAM and PEG 350 - 3.0 PAMAM was investigated. Light test was employed to evaluate the influse of PEG 350 - 3.0 PAMAM on the photo - stability of CPT. RESULTS The solubility, photostability and release rate of CPT were increased in PEG 350 - 3.0 PAMAM solution in comparison with that in G 3.0 PAMAM solution. CONCLUSION These studies indicated that PEG 350 - 3.0 PAMAM might be a potential carrier of CPT as a novel drug delivery system.

关 键 词：PEG350—3.0PAMAM 喜树碱 增溶 释放 光敏性 

分 类 号：R944.9[医药卫生—药剂学]