Center for Bionanoengineering and State Key Laboratory of Chemical Engineering, Department of Chemical and Biochemical Engineering, Zhejiang University, Hangzhou, 310027, PR China.
Chemistry. 2011 May 2;17(19):5319-26. doi: 10.1002/chem.201003495. Epub 2011 Apr 4.
Poly(β-aminoester) dendrimers have been prepared. These systems represent the first degradable dual pH- and temperature-responsive dendrimers displaying photoluminescence. The pH/temperature sensitivities are interrelated; the lower critical solution temperature of the dendrimer decreases as the pH of the solution is increased. The sensitivities are mainly due to phase changes of the surface groups with changes in pH or temperature. These dual-responsive dendrimers are very useful in drug delivery. They may be loaded with a hydrophobic drug at low temperature without using organic solvents. The loaded drug is released very slowly and steadily at 37 °C and physiological pH, but can be quickly released at acidic pH, for example the lysosomal pH (pH 4-5), for intracellular drug release. These dendrimers also display strong photoluminescence, which can be exploited for monitoring drug loading and release. Thus, poly(β-aminoester) dendrimers constitute ideal drug carriers since their thermal sensitivity allows the loading of drugs without using organic solvents, their pH sensitivity permits fast intracellular drug release, and their photoluminescence provides a means of monitoring drug loading and release.
聚（β-氨基酯）树状大分子已被制备。这些体系代表了首例可降解的双重 pH 和温度响应树状大分子，具有光致发光性能。pH/温度的响应性是相互关联的；随着溶液 pH 值的增加，树状大分子的低临界溶液温度降低。这些响应性主要归因于表面基团的相变化随 pH 或温度的变化。这些双重响应性树状大分子在药物传递中非常有用。它们可以在低温下装载疏水性药物，而无需使用有机溶剂。在 37°C 和生理 pH 值下，负载的药物可以缓慢而稳定地释放，但在酸性 pH 值下（例如溶酶体 pH 值为 4-5），可以快速释放，用于细胞内药物释放。这些树状大分子还显示出很强的光致发光性，可用于监测药物的负载和释放。因此，聚（β-氨基酯）树状大分子是理想的药物载体，因为其热敏感性允许在不使用有机溶剂的情况下装载药物，其 pH 敏感性允许快速的细胞内药物释放，而其光致发光提供了监测药物负载和释放的手段。
