An AIEgen and Iodine Double‐Ornamented Platinum(II) Complex for Bimodal Imaging‐Guided Chemo‐Photodynamic Combination Therapy

Abstract Real‐time biodistribution monitoring and enhancing the therapeutic efficacy of platinum(II)‐based anticancer drugs are urgently required to elevate their clinical performance. Herein, a tetraphenylethene derivative (TP) with aggregation‐induced emission (AIE) properties and an iodine atom are selected as ligands to endow platinum (II) complex TP‐Pt‐I with real‐time in vivo self‐tracking ability by fluorescence (FL) and computerized tomography (CT) imaging, and improved anticancer efficacy by the combination of chemotherapy and photodynamic therapy. Especially, benefiting from the formation of a donor‐acceptor‐donor structure between the AIE photosensitizer TP and Pt‐I moiety, the heavy atom effects of Pt and I, and the presence of I, TP‐Pt‐I displayed red‐shifted absorption and emission wavelengths, enhanced ROS generation efficiency, and improved CT imaging capacity compared with the pristine TP and the control agent TP‐Pt‐Cl. As a result, the enhanced intratumoral accumulation of TP‐Pt‐I loaded nanoparticles is readily revealed by dual‐modal FL and CT imaging with high contrast. Meanwhile, the TP‐Pt‐I nanoparticles show significantly improved tumor growth‐inhibiting effects on an MCF‐7 xenograft murine model by combining the chemotherapeutic effects of platinum(II) and the photodynamic effects of TP. This self‐tracking therapeutic complex thus provides a new strategy for improving the therapeutic outcomes of platinum(II)‐based anticancer drugs.