Biofunctionalization of β-cyclodextrin nanosponges using cholesterol

Abstract

Cyclodextrins nanosponges (CD-NSPs) are highly microporous crosslinked polymers with potential applications in the delivery of small and macro-molecular therapeutic agents. Despite the potent host-guest inclusion property, their inherent lack of cellular binding ability has limited applications in drug delivery. Herein, we functionalized the surface of β-cyclodextrin nanosponge (β-CD-NSP) with cholesterol, which is endogenous physiological molecules, widely distributed in all cells, and responsible for cell interactions and protein binding. The surface grafting of synthesized β-CD-NSP was confirmed with spectroscopic, microscopic, thermogravimetric, and chromatographic techniques. Moreover, β-CD-NSP was found to be safe in cytotoxicity assay. Doxorubicin (Dox) was selected as a model drug for drug adsorption study of cholesterol hydrogen succinate (CHS) grafted β-CD-NSP. The cellular uptake of NSP was found to be enhanced after CHS modification confirmed by confocal laser scanning microscopy (CLSM). Thus, proposed CHS modified β-CD-NSP system could be used as a site-specific drug delivery carrier.

Keywords: Biofunctionalization; Cellular uptake; Cholesterol; β-CD nanosponge.