Stimulus-responsive supramolecular vesicles with effective anticancer activity prepared by cyclodextrin and ftorafur

Vesicles directly prepared from cyclodextrin–ftorafur supramolecular amphiphiles were reported. Ftorafur can be efficiently encapsulated in the cyclodextrin cavities embedded in the vesicle membrane. The morphologies and diameters of the vesicles were identified in detail by transmission electron microscopy (TEM), scanning electron microscopy (SEM), atomic force microscopy (AFM) and dynamic light scattering (DLS). X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), UV–vis spectrum, 1H NMR and 2D NMR ROESY were further employed to study the formation mechanism of the vesicles. Various morphologies were detected when different host molecules were employed as the hydrophilic moieties of the vesicles’ building blocks. Copper ions could arouse the simultaneous release of ftorafur from the vesicles. The proliferation and cell cycle assay of colon carcinoma cell Line HT-29 were performed to evaluate the anticancer effects of the ftorafur-loaded vesicles and natural ftorafur, respectively. The ftorafur-loaded vesicle system exhibits a better anticancer effect than the sole ftorafur.