聚酰胺—胺树枝状高分子/喜树碱复合物的制备及体外释放研究

Preparation and in vitro Release of Camptothecin Complexation with Polyamidoamine

利用聚酰胺—胺树枝状高分子与喜树碱的静电复合作用进行复合,以水为溶剂,第四、五代聚酰胺—胺树枝状高分子为载体采用搅拌法进行复合,探讨其作为抗肿瘤药物载体的可能性.应用紫外分光光度法(UV)测定复合量,采用高效液相色谱法(HPLC)测定其在PBS中的释放特性.喜树碱在聚酰胺—胺树枝状高分子水溶液中内酯环开环,溶解度增大,在PBS中并无明显的缓释效果.结果表明聚酰胺—胺树枝状高分子不宜作为具内酯环,遇碱不稳定药物的载体.

To investigate polyamidoamine （PAMAM） as a potential drug delivery carrier for camptotheein,complexes of the fourth and fifth generation PAMAM/Camptotheein were pre- pared in water by stirring method. The amounts of drug loading were determined by UV,and the release profile by I-IPLC in phosphate buffer solutions. The solubility of Camptothecin enhanced in PAMAM solutions and there were no obvious sustained release effects in PBS. PAMAM could not be used as carriers of unstable drug in weak base condition and hydrophilic drug.