A nano-cocktail of an NIR-II emissive fluorophore and organoplatinum(ii) metallacycle for efficient cancer imaging and therapy

The scarcity of efficient imaging technologies for precise cancer treatment greatly drives the development of new nanotheranostic based platforms that enable both diagnostic and therapeutic functions, together in a single formulation. Owing to the complicated physiological microenvironment, nanosystems designed with the possibility of noninvasive real-time monitoring of therapeutic progression in the second near-infrared channel (NIR-II, 1000-1700 nm) could substantially improve the current cancer therapies. Herein, we design a novel NIR-II theranostic nanoprobe, PSY (size ∼110 nm), by incorporating organoplatinum(ii) metallacycles P1 and an organic NIR-II molecular dye, SY1030, into the FDA-approved polymer Pluronic F127. Preliminary in vitro and in vivo studies suggest that PSY is capable of being internalized into glioma U87MG-cells with no significant internalization in non-cancerous tissues. In addition, it shows excellent photostability and minimal background for real-time monitoring the process of therapy in the NIR-II region. Furthermore, in U87MG xenografts and orthotopic breast tumor, PSY demonstrat significantly improved anticancer efficacy compared to a clinically approved Pt(ii)-based anticancer drug, cisplatin. The engineered nano-cocktail PSY offers a simple strategy for delivering the organoplatinum(ii) macrocycle P1 and NIR-II fluorophore SY1030 as a cocktail of diagnostic and therapeutic functions and highlights its promising capacity for future cancer treatment.