Nanoregulators Inhibiting Tyrosinase to Synergistically Enhance the Efficacy of Melanoma Photodynamic Therapy

ABSTRACT Photodynamic therapy (PDT) is a promising therapeutic way for melanoma with noninvasiveness, but its efficiency is often affected by tumor‐intrinsic melanin, limiting light usage and weakening ROS‐induced cytotoxicity. Here, we developed CeTI nanoparticles (CeTI NPs) to co‐deliver Ce6 and a tyrosinase inhibitor (TI) with the assistance of DSPE‐mPEG. CeTI NPs were able to generate ROS under light illumination and released TI effectively under acidic conditions. In vitro results demonstrated CeTI NPs possessed excellent photo‐toxicity to kill B16F10 cells effectively by generating intracellular ROS and further inducing cellular apoptosis. In vivo results showed CeTI NPs inhibited tumor growth efficiently while maintaining excellent bio‐safety. Overall, this work provides a potential way in clinic to relieve melanin‐associated resistance and amplify PDT outcomes in melanoma treatment.