Photodynamic therapy (
PDT) utilizes the photogeneration of
reactive oxygen species (ROS) with high cytotoxicity to kill
cancer cells, holding great promise for
cancer treatment. Fractionated delivery of
singlet oxygen (1O2) is a wise approach to relieving
hypoxia, thus enhancing the therapeutic efficacy. In this article, an
anthracene-functionalized semiconducting compound (DPPA) has been designed and synthesized. With irradiation, the compound is able to undergo efficient intersystem crossing (ISC) and non-radioactive decay for photodynamic/photothermal synergistic
therapy. In addition, the
anthracene module is able to capture and release 1O2 reversibly with or without irradiation. DPPA nanoparticles (NPs) obtained by nanoprecipitation with
DSPE-PEG exhibit considerable high
phototoxicity on human
kidney cancer cells (A498), and the half maximum inhibitory concentration (IC50) is 15.8 μg/ml. Furthermore, an in vivo study demonstrates that complete
tumor suppression was observed when the mice were administered DPPA NPs with the help of
laser, compared with the control and dark groups. The H&E analysis of the normal tissues (the heart, liver, spleen, lungs, and kidney) indicates that such NPs cause no side effects, indicating the biosafety of DPPA NPs. The results provide a strategy to design a heavy-atom-free
photosensitizer for photothermal and fractionated
PDT against kidney
tumors.