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.

中文翻译：

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β- D-半乳糖修饰的支柱[5]芳烃和喜树碱前药构建的GSH响应性超分子纳米颗粒可用于靶向抗癌药物递送

具有靶向性和刺激响应性的药物递送系统的超分子构建仍然是一项艰巨的任务。在此，通过β- D-半乳糖功能化的水溶性支柱[5]芳烃（GalP5）和含有喜树碱前药（G）的二硫键之间的主体-客体络合，构建了GSH反应性超分子前药纳米颗粒。所获得的前药纳米颗粒在生理条件下是稳定的，而在具有高GSH浓度的模拟肿瘤环境中触发了有效的药物释放。体外研究表明，由于半乳糖单位的主动靶向作用，这些前药纳米颗粒优先进入过唾液酸糖蛋白受体过表达的HepG2细胞。这种主动的靶向作用使抗癌功效最大化，并减少了正常细胞的不良副作用。