聚酰胺-胺(PAMAM)树状大分子对甲氨蝶呤的包合及缓释研究

Complex and in vitro Release of Methotrexate-PAMAM Dendrimer

以甲氨蝶呤 (MTX)为模型药物 ,研究了 G5 .0 PAMAM树状大分子对其包合和释放 ,并用 1 3C NMR对 PAMAM-MTX包合物进行了表征 .UV-Vis研究结果表明 ,1个 G5 .0 PAMAM树状大分子能包合 2 7个MTX分子 ,体外释放研究表明 ,在 3 7℃ ,p H=7.4的 1 0 mmol/LTris-HCl缓冲溶液中 G5 .0 PAMAM树状大分子对 MTX具有明显的缓释作用 .

We investigated the interaction between G5\^0 PAMAM and methotrexate(MTX) drug molecules by 13C NMR, and it has been proven that the interaction is occurring between the PAMAM amine functional groups and the MTX carboxyl groups. UV-Vis study showed each G5.0 PAMAM could conjugate up to 27 MTX molecules. The release of MTX from complex is much slower than that of free MTX at pH=7.4, 10 mmol/L Tris-HCl buffer. The presence of 0.02 mol/L NaCl in buffer increases the release rate of MTX from the complex, which further defines the interaction between PAMAM and MTX.