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Camptothecin, as an antitumor drug, has shown significant antitumor activity against various cancers through the inhibition of topoisomerase I. However, its poor solubility severely limits the clinical applications. Here, we report a camptothecin supramolecular vesicle based on the host–guest interactions, which can uniformly disperse camptothecin into water and greatly enhance camptothecin aqueous solubility. The camptothecin vesicles were identified by transmission electron microscopy (TEM), scanning electron microscopy (SEM), and dynamic light scattering (DLS). X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), UV–vis spectrum, 1 H NMR and 2D NMR ROESY were further employed to study the formation mechanism of the vesicles. Furthermore, camptothecin could be controllably released when the competitive guests were added into the vesicles system. Finally, the camptothecin vesicles in aqueous solution exhibited comparable antitumor activity in vitro as natural camptothecin in DMSO to HeLa cells under the same conditions. [ABSTRACT FROM AUTHOR]

Curcumin is a safe and nontoxic natural potential antitumor drug. However, its extremely low aqueous solubility severely limits its clinical application. We designed a supramolecular curcumin vesicle based on different curcumin-cyclodextrin amphiphiles, which could greatly enhance the aqueous solubility of curcumin up to 7000-fold. The vesicles can exist for about one month in aqueous solution at around 20 °C, showing a certain colloidal stability. The curcumin-β-cyclodextrin vesicles were identified 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 and 1 H NMR were further employed to study the formation mechanism of the vesicles. Curcumin vesicles were also prepared when different host molecules were employed as the hydrophilic heads of the supramolecular amphiphiles. Finally, curcumin could be controllably released with the disruption of the vesicles when the external stimuli, including competitive guest molecules, enzymes and copper ions were added into the vesicles system. [ABSTRACT FROM AUTHOR]