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.
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