Key Laboratory of Functional Polymer Materials (Ministry of Education), Institute of Polymer Chemistry, Nankai University, Tianjin, China.
Bioconjug Chem. 2010 Sep 15;21(9):1596-601. doi: 10.1021/bc900490u.
To improve the efficacy and bioacceptability of polyamidoamine (PAMAM) in potential biomedical applications, the PAMAM dendrimers (first generation) were partially modified with cholic acid. (1)H NMR studies and acid-base titration show that two cholic acid molecules are linked to one PAMAM. The modified PAMAM dendrimers self-assemble to form dendritic multimolecular micelles in aqueous solutions, with a diameter of 120 nm measured by dynamic light scattering. These micelles can encapsulate hydrophobic drug molecules in aqueous media and exhibit pH sensitivity. The in vitro results demonstrate that the anticancer activity of camptothecin is significantly enhanced at low drug dose after being encapsulated by these micelles in the presence of serum. Therefore, the dendritic multimolecular micelles based on low generation dendrimers may have potential applications in the delivery of drugs.
为提高聚酰胺-胺（PAMAM）在潜在生物医学应用中的疗效和生物可接受性，用胆酸对 PAMAM 树枝状大分子（第一代）进行了部分修饰。（1）H NMR 研究和酸碱滴定表明，两个胆酸分子与一个 PAMAM 相连。修饰后的 PAMAM 树枝状大分子在水溶液中自组装形成树枝状多分子胶束，用动态光散射法测量其直径为 120nm。这些胶束可以在水介质中包裹疏水分子药物，并表现出 pH 敏感性。体外实验结果表明，在血清存在的情况下，这些胶束包封喜树碱后，药物剂量较低时，其抗癌活性显著增强。因此，基于低代树枝状大分子的树枝状多分子胶束在药物传递方面可能具有应用潜力。
