Dual acid-responsive bola-type supramolecular vesicles for efficient intracellular anticancer drug delivery

Abstract

Dual acid-responsive bola-type supramolecular vesicles have been successfully constructed for efficient intracellular anticancer drug delivery, which are fabricated by the complexation between a water-soluble pillar[5]arene (WP5) and an acid-sensitive guest molecule (G) containing the 2,4,8,10-tetraoxaspiro[5.5]undecane moiety. Compared with the control system that only has single pH-responsiveness of WP5, the obtained dual acid-responsive supramolecular vesicles exhibit much faster drug release efficiency under the acid microenvironment of cancer cells. Moreover, cytotoxicity experiments confirm that the doxorubicin (DOX)-loaded supramolecular vesicles can not only obviously enhance the anticancer efficiency of free DOX for tumor cells, but also remarkably reduce the side effects on normal cells, suggesting their potential applications in cancer therapy.