Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
Macromol Biosci. 2012 Oct;12(10):1375-83. doi: 10.1002/mabi.201200122. Epub 2012 Aug 27.
The pH sensitivity of a series of PbAEs synthesized from primary amines and diacrylates is studied. By changing alkyl groups of the amine monomers, the pKb can be tuned across a broad range (from 3.5 to 7.2). Micelles formed from a PEG-PbAE block copolymer retain the pH sensitivity of PbAE and can stably load hydrophobic molecules under neutral pH, while quickly dissociate and release their cargoes at pH ≈ 6.0. When the chemotherapy drug DOX is loaded, the micelles show efficient cell proliferation inhibition to HeLa cells and fast intracellular release. Thus, the primary-amine-based PbAEs are shown to be promising in the construction of intracellular targeting drug delivery systems.
研究了一系列由伯胺和二丙烯酸酯合成的 PbAEs 的 pH 敏感性。通过改变胺单体的烷基基团，可以在很宽的范围内调节 pKb（从 3.5 到 7.2）。由 PEG-PbAE 嵌段共聚物形成的胶束保留了 PbAE 的 pH 敏感性，并且可以在中性 pH 下稳定地负载疏水分子，而在 pH ≈ 6.0 时快速解离并释放其货物。当负载化疗药物 DOX 时，胶束对 HeLa 细胞显示出有效的细胞增殖抑制作用和快速的细胞内释放。因此，基于伯胺的 PbAEs 在构建细胞内靶向药物输送系统方面具有广阔的应用前景。
