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An Iridium (III) Complex Bearing a Donor–Acceptor–Donor Type Ligand for NIR-Triggered Dual Phototherapy
Authors:Jian Zhao  Kaiwen Yan  Gang Xu  Xue Liu  Qiang Zhao  Chenjie Xu  Shaohua Gou
Affiliation:1. Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research and Pharmaceutical Research Center, School of Chemistry and Chemical Engineering, Southeast University, Nanjing, 211189 China;2. Key Laboratory for Organic Electronics and Information Displays, Institute of Advanced Materials, Nanjing University of Posts and Telecommunications, Nanjing, 210023 China;3. Department of Biomedical Engineering, City University of Hong Kong, 83 Tat Chee Avenue, Kowloon, Hong Kong SAR, China
Abstract:Iridium(III) complexes are an important group of photosensitizers for photodynamic therapy (PDT). This work constructs a donor–acceptor–donor structure-based iridium(III) complex (IrDAD) with high reactive oxygen species (ROS) generation efficiency, negligible dark toxicity, and synergistic PDT and photothermal therapy (PTT) effect under near-infrared (NIR) stimulation. This complex self-assembles into metallosupramolecular aggregates with a unique aggregation-induced PDT behavior. Compared with conventional iridium(III) photosensitizers, IrDAD not only achieves NIR light deep tissue penetration but also shows highly efficient ROS and heat generation with ROS quantum yield of 14.6% and photothermal conversion efficiency of 27.5%. After conjugation with polyethylene glycol (PEG), IrDAD is formulated to a nanoparticulate system (IrDAD-NPs) with good solubility. In cancer phototherapy, IrDAD-NPs preferentially accumulate in tumor area and display a significant tumor inhibition in vivo, with 96% reduction in tumor volume, and even tumor elimination.
Keywords:cancer therapy  donor–acceptor ligand  iridium complex  photodynamic therapy  photothermal therapy
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