Efficient anticancer drug delivery using nano-colloids self-assembled with an unconventional amphiphile bearing pumpkin-shaped host molecule

Abstract

A new type of amphiphiles bearing macrocycle such as cucurbit[7]uril (CB[7]) spontaneously forms a nanomaterial in water, specifically vesicles (tACB[7] vesicles) with a positive surface charge, verified through various analytical techniques including TIRF, DLS and TEM. Functional validation not only reveals the accessibility of the CB[7] portal on these vesicles allowing CB[7]-based host-guest interactions with various functional guest molecules such as fluorescein isothiocyanate conjugated adamantylammonium and spermine (FITC-AdA and FITC-SPM, respectively) using confocal laser scanning microscopy, but also showcases the effective internalization of tACB[7] vesicles into cancer cells with the anticancer drug oxaliplatin (OxPt), as a guest to CB[7], through in vitro cell experiments. Hence, this study provides a blueprint to impart amphiphilic properties to CB[7] through synthetic design and highlights the potential of CB[7] derivatives as a new class of unconventional amphiphiles self-assembling into functional nanomaterials for advanced drug delivery.