10-羟基喜树碱-癸二酸-LDH杂化物的制备及性能

采用二次插层法成功制备了10-羟基喜树碱(HCPT)-癸二酸(SC)插层的层状双金属氢氧化物(LDH). 先采用共沉淀法制备SC柱撑LDH杂化物(SC-LDH), 再在乙醇介质中将HCPT插入LDH层间形成HCPT-SC-LDH纳米杂化物. 依据SC和HCPT的分子尺寸和纳米杂化物的通道高度, 推测SC分子在层间可能为双层排列, SC分子两端的羧基同时键合在同一个LDH层片表面上; HCPT分子插入(或溶入)SC分子碳氢链形成的疏水区中. 所制备的纳米杂化物既可稳定HCPT的内酯环, 又可明显提高HCPT的溶解度, 还具有明显的药物缓释效果, 其释放动力学过程符合准二级动力学方程.

Synthesis and Characterization of 10-Hydroxyl Camptothecin-Sebacate-LDH Nanohybrid

The nanohybrid of 10-hydroxyl camptothecin(HCPT)-sebacate(SC)-intercalated layered double hydroxide(LDH), HCPT-SC-LDH, was prepared by a secondary intercalation method. First, the nanohybrid of SC intercalated Mg2Al-NO3 LDH was prepared by a co-precipitation method; second, HCPT was intercalated into the LDH's gallery in ethanol medium. According to the gallery height of the SC-LDH sample and the size of SC molecule, a probably morphology of the SC molecules in the gallery of LDH was suggested that the SC molecules arranged as a bilayer structure in which two carboxylate groups of SC molecule combined onto one LDH layer surface. And HCPT was intercalated into the LDH's gallery via hydrophobic interaction. The encapsulated HCPT could keep biologically active lactone structure, and the nanohybrid could improve the HCPT solubility. Moreover, the obtained HCPT-SC-LDH nanocomposites showed obvious controlled release and the release in vitro of HCPT could be fitted with the pseudo-second-order model.