(聚酰胺-胺)树状大分子对甲氨蝶呤的复合和释放研究  

INVESTIGATION OF PAMAM DENDRIMER_MTX COMPLEX:FORMATION AND in vitro RELEASE

作　　者：叶玲[1] 杨华[1] 何满林[1] 唐亚娟[1] 陈双玲[1] 原阳[1] 恽榴红[2] 

机构地区：[1]首都医科大学生物学与药学院,北京100054 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《高分子学报》2006年第1期32-36,共5页Acta Polymerica Sinica

基　　金：北京市科技新星(项目号954812000);北京市教委科技发展计划(项目号00KJ-107)资助项目

摘　　要：以甲氨蝶呤(MTX)为模型药物,研究了PAMAM与MTX的复合及体外释放.1H-,13C-NMR数据表明MTX与PAMAM树状大分子形成复合物是由于MTX羧基和PAMAM树状大分子外端氨基之间的相互作用.该复合物在pH=7.4,10 mmol/L Tris-HCl中非常稳定,表现出明显的缓释效果.当溶液中的离子强度增加时,会破坏PAMAM-MTX复合物的稳定性,缓释作用部分或全部失去,说明PAMAM树状大分子与MTX之间的相互作用属于静电作用.UV测得每个G5.0 PAMAM、G4.0 PAMAM树状大分子分别能复合271、4个MTX分子.The mechanism of formation of polyamidoamine （PAMAM） dendrimer-methotrexate （MTX） complex and the release behaviors of MTX from the complex have been investigated. ^1H-, ^13 C-NMR data confirmed that the formation of PAMAM-MTX complex was due to the interaction between PAMAM external amino groups and the MTX carboxyl groups. The PAMAM-MTX complex was stable in 10 mmol/L, pH 7.4 tris-HC1 buffer solution. However, with increasing the ionic strength in the buffer solution, it was easier for MTX to escape from the complex, which suggested that the interaction between PAMAM and MTX was electrostatic in nature. UV results demonstrated that the higher the generation of PAMAM, the greater its capacity to carry MTX molecules, e. g. G. 5.0 PAMAM and G4.0 PAMAM could load 27 and 14 MTX molecules,respectively.

关 键 词：PAMAM树状大分子 甲氨蝶呤 复合 释放 

分 类 号：TQ460.1[化学工程—制药化工]