Photodynamic therapy (PDT) relying on photosensitizer-induced production of reactive oxygen species (ROS) for killing cancer cells has emerged as a non-invasive anti-cancer strategy. Compared with oxygen-dependent type-II photosensitizers (PSs) for PDT, the development of intrinsic oxygen-independent type-I ones is highly desired but remains a challenge. In this work, two netural Ir(III) complexes that can produce type-I reactive oxygen species, namely MPhBI-Ir-BIQ (Ir-1) and NPhBI-Ir-BIQ (Ir-2), were synthesized. Bright deep-red emitting nanoparticles with moderate particle size are beneficial for imaging-guided PDT. In in vitro experiments, importantly, the excellent biocompatibility, the targeting of lipid droplets (LDs), and the type-I ⋅OH and O ⋅ generation promoted effective photodynamic activity. This work will guide the building of type-I Ir(III) complexes PSs and can provide advantages for potential clinical applications under hypoxic conditions.
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