Supramolecular nanoprodrug based on a chloride channel blocker and glycosylated pillar[5]arenes for targeted chemoresistance cancer therapy

A supramolecular nanoprodrug (DOX@GP5 superset of Pro-NFA) was constructed based on the host-guest complexation of chloride channel blocker prodrug (Pro-NFA) and glycosylated pillar[5]arene (GP5), which could target tumor cells via galactose and release DOX/NFA responsively under esterase stimulation. In vitro studies revealed that this supramolecular nanoprodrug can overcome drug resistance through inhibiting chloride channels as well as inhibiting the migration of HepG2/ADR cells. This strategy can therefore achieve enhanced potency in chemotherapy through reverse chemoresistance.

Automated summary

A supramolecular nanoprodrug (DOX@GP5 Pro-NFA) was developed, which could target tumor cells and release DOX/NFA responsively. The nanoprodrug showed the ability to overcome drug resistance through inhibiting chloride channels and inhibiting cell migration. This strategy can enhance chemotherapy potency through reverse chemoresistance.