Key Laboratory of Mesoscopic Chemistry of MOE and Collaborative Innovation Center of Chemistry for Life Sciences, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing, 210023, China.
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing, 210023, China.
Chem Commun (Camb). 2017 Jul 27;53(61):8596-8599. doi: 10.1039/c7cc04932c.
Supramolecular construction of a targeted and stimuli-responsive drug delivery system is still a challenging task. Herein, GSH-responsive supramolecular prodrug nanoparticles were constructed by the host-guest complexation between a β-d-galactose-functionalized water-soluble pillar[5]arene (GalP5) and a disulfide bond containing camptothecin prodrug (G). The obtained prodrug nanoparticles were stable under physiological conditions, whereas efficient drug release was triggered in a simulated tumor environment with high GSH concentration. In vitro studies revealed that these prodrug nanoparticles preferentially entered asialoglycoprotein receptor-overexpressing HepG2 cells due to the active targeting effect of galactose units. This active targeting effect resulted in the maximization of anticancer efficacy and reduction of the undesirable side effects to normal cells.
超分子构建靶向和刺激响应型药物传递系统仍然是一项具有挑战性的任务。在此，通过β-D-半乳糖功能化水溶性柱[5]芳烃（GalP5）与含有二硫键的喜树碱前药（G）之间的主客体络合作用，构建了 GSH 响应性超分子前药纳米粒子。所得前药纳米粒子在生理条件下稳定，而在具有高 GSH 浓度的模拟肿瘤环境中则触发了有效的药物释放。体外研究表明，由于半乳糖单元的主动靶向作用，这些前药纳米粒子优先进入过表达去唾液酸糖蛋白受体的 HepG2 细胞。这种主动靶向作用使抗癌功效最大化，并减少了对正常细胞的不良副作用。
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