Abstract
Abstract Photodynamic therapy (PDT) is of great interest as an emerging paradigm towards cancer treatment, owing to its advantages of minimal invasiveness and low toxicity. In this work, we incorporated cisplatin into an AIE-based photosensitizer (BT) and achieved a highly efficient antitumor drug (BT-Pt). Possessing AIE characteristics, BT-Pt exhibited NIR fluorescence with large Stokes shift in cells, which can guide the location of the drug. More importantly, the ROS generation efficiency of BT-Pt has extremely been promoted with the fabrication of cisplatin, compared with BT. As a result, BT-Pt demonstrated favorable therapeutic efficacy with a half maximal inhibitory concentration (IC50) value of 1.54 μM for HeLa cells upon white light irradiation, attributed to its synergetic PDT and chemotherapy. The design strategy of such platinated photosensitizer showed great potential in developing multifunctional anticancer drugs with combinatorial photodynamic–chemotherapy, especially when ablating cisplatin resistant cancer cells and hypoxic tumors.
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