Self-Illuminated PDT Platform for Highly Specific Diagnosis and Therapeutics for Deep Sited Tumor

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Early diagnosis and treatment of cancer have attracted extensive attention, however, there is still a shortage of techniques that integrate tumor imaging and therapeutics. Photodynamic therapy (PDT) that involves functional photosensitive dyes has been considered as a potential solution. PDT mainly relies on light-activated photosensitizers (PSs) to (1) visually label cancer with luminescence and (2) generate excessive toxic reactive oxygen species (ROS). However, one of the main reasons that hinders PDT application is the limited tissue penetration of excitation light. Hence, solving the excitation problems of PSs in deep sites and overcome the tissue obstacles are of great significance for efficient all-in-one cancer diagnosis and treatment. This project will develop a Multi-Function Integrated Self-Illuminated PDT platform that can overcome the limited light penetration in conventional PDT, enabling synchronous diagnosis and treatment of orthotopic tumors. BODIPY-luminol dyads will be constructed by connecting BODIPY PSs (with long triplet lifetime) with afterglow luminol. Upon triggered by the specific tumor microenvironment (TME), the dyads can be activated by chemical energy to singlet excited state (S1), then undergointersystem crossing to triplet excited state, where the dyad sensitize O2 to yield 1O2 for PDT. The PDT process relies on the chemical reaction between luminol and TME and can get rid of the penetration limitation of traditional external light. Meanwhile, the dyad can generate chemiluminescence from S1, showing the potential of early cancer imaging owing to its inborn background-free characteristics. The outcomes of this project are expected to provide possibilities of early detection and intervention of cancer and reducing the obstacles of clinical transformation to improve patient survival.