Key Laboratory of Biomedical Polymers of Ministry of Education, Department of Chemistry, Wuhan University, Wuhan, Hubei, People's Republic of China.
ACS Appl Mater Interfaces. 2015 Jul 22;7(28):15148-53. doi: 10.1021/acsami.5b03866. Epub 2015 Jul 13.
Drug delivery has become an important strategy for improving the chemotherapy efficiency. Here we developed a multifunctionalized nanosized albumin-based drug-delivery system with tumor-targeting, cell-penetrating, and endolysosomal pH-responsive properties. cRGD-BSA/KALA/DOX nanoparticles were fabricated by self-assembly through electrostatic interaction between cell-penetrating peptide KALA and cRGD-BSA, with cRGD as a tumor-targeting ligand. Under endosomal/lysosomal acidic conditions, the changes in the electric charges of cRGD-BSA and KALA led to the disassembly of the nanoparticles to accelerate intracellular drug release. cRGD-BSA/KALA/DOX nanoparticles showed an enhanced inhibitory effect in the growth of αvβ3-integrin-overexpressed tumor cells, indicating promising application in cancer treatments.
药物递送已成为提高化疗效率的重要策略。在这里，我们开发了一种多功能纳米白蛋白药物递送系统，具有肿瘤靶向、细胞穿透和内体溶酶体 pH 响应特性。cRGD-BSA/KALA/DOX 纳米粒通过静电相互作用自组装而成，其中细胞穿透肽 KALA 与 cRGD-BSA 相互作用，cRGD 作为肿瘤靶向配体。在内涵体/溶酶体酸性条件下，cRGD-BSA 和 KALA 的电荷变化导致纳米粒解体，从而加速细胞内药物释放。cRGD-BSA/KALA/DOX 纳米粒在过表达 αvβ3 整合素的肿瘤细胞生长中表现出增强的抑制作用，表明其在癌症治疗中有很好的应用前景。
