【摘要】 目的探讨了聚酰胺-胺(PAMAM)树状大分对抗癌药物甲氨蝶呤体外释放作用及其释放机制。方法采用紫外分光光度法测定G(代)4.0PAMAM树状大分子对抗癌药物甲氨蝶呤(MTX)的复合和缓释作用。用磁共振谱和氢谱探讨其复合的机制。结果G4.0PAMAM树状大分子能复合14个MTX分子;G4.0PAMAM树状大分子-MTX复合物在10mmol/LTris-HCl溶液中释放80%MTX需要200h,缓释效果是对照(游离MTX)的10倍;随着介质浓度的增加,G4.0PAMAM树状大分子-MTX复合物缓释效果降低,其稳定性也降低。结论1HNMR和13CNMR数据表明G4.0PAMAM树状大分子与MTX通过PAMAM树状大分子氨基阳离子与MTX羧基阴离子之间的静电作用而形成复合物。更多还原

【Abstract】 Objective Dendrimer, a new class polymeric materials of highly branched, symmetric and nanoscale, are considered as potential drug delivery vehicle for their particular structure and character. The capability of G4.0 Polyamidoamie (PAMAM) dendrimer as anticancer drug methotrexate (MTX) carrier were studied. Methods UV has been employed to monitor the in vitro release of MTX from G4.0 PAMAM in different buffers. We discuss mechanism of complex by 1H and 13 C NMR. Results Each G4.0 PAMAM could conjugated 14 MTX molecules; An electronic interaction between G4.0 PAMAM primary amine groups and MTX carboxylic groups was demonstrated by 1H and 13 C NMR. It took 200 h to release 80% MTX from the G4.0 PAMAM-MTX complex in 10 mmol/L, pH 7.4 Tris-HCl buffer solution, while 20 h for pure MTX under same condition; With the increasing of ionic strength in Tris-HCl buffer solution, the G4.0 PAMAM-MTX complex released MTX fast and the stability of the G4.0 PAMAM-MTX system decreased. Conclusion 1H and 13 C NMR data demonstrated the interaction between G4.0 PAMAM dendrimer primary amine groups and MTX carboxylic groups is due to the electrostatic force; G4.0 PAMAM dendrimer could load 14 MTX molecules; the controlled release ability of G4.0 PAMAM-MTX complex was 10 times better than the control (pure MTX) in 10 mmol/L(pH 7.4) Tris-HCl buffer solution.更多还原