A quinolone derivative-based organoplatinum(II) metallacycle supramolecular self-delivery nanocarrier for combined cancer therapy

Optimised drug delivery systems with low toxicity and high efficacy for suppressing cancer cells are urgently needed. In this study, a quinolone derivative-based organoplatinum(II) supramolecular coordination complex (SCC) was synthesised by [2 + 2] coordination-driven self-assembly. Using this molecular design, synergistic chemotherapeutic effects were achieved by combining the anticancer agent platinum acceptor and quinolone derivative at a fixed ratio. Importantly, the well-defined rhomboidal shape and size of the SCC metallacycle self-assembled into nanoparticles with an average diameter of 38 nm in aqueous solution, conferring improved passive targeting and internalisation abilities towards tumour cells via the enhanced permeability and retention effect. In vitro evaluation with HepG2 cells showed that integration of the quinolone derivative and organoplatinum(II) acceptor improved antitumor activity compared with each independent component. These properties reveal the potential of Pt(II)-based SCCs for use in antitumor applications as a supramolecular chemotherapy self-delivery platform.A Pt(II) metallacycle-based supramolecular self-delivery nanocarrier platform through coordination-driven self-assembly of a dipyridine-functionalised quinolone derivative donor (QD) and 60° Pt (II) acceptor (PhenPt) was successfully constructed. This nanocarrier considerably enhanced the internalisation and anticancer efficacy, as shown by in vitro studies.