A host-guest drug delivery nanosystem for supramolecular chemotherapy

Supramolecular chemotherapy is currently a new strategy to improve the therapeutic efficacy as well as overcome the side effects of traditional chemotherapy. Herein, a supramolecular chemotherapy platform based on the pegylated guanidinium-modified calix[5]arene pentadodecyl ether (GC5A-12C) nanoassembly was prepared. Three commercially available antitumor drugs: oxaliplatin, methotrexate and chlorambucil, all showed strong binding to this GC5A-12C nanocarrier. The supramolecular nanodrugs achieved higher anticancer performances compared with free drugs in cell experiments. Furthermore, the cellular uptake mechanisms and efficacy are confirmed by fluorescence imaging. [Display omitted] •A host-guest drug delivery nanosystem is fabricated for supramolecular chemotherapy.•The GC5A-12C nanocarrier as a universal platform can load various drugs via the host-guest complexation.•GC5A-12C nanocarriers’ drug loading and encapsulation efficiency are higher than liposomes due to host-guest interactions•GC5A-12C nanocarriers promote the cellular uptake of drugs, leading to higher cytotoxicity to cancer cells than free drug.