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Photodynamic therapy (PDT) is a minimally invasive tumor targeting strategy, in which tumor tissues can be selectively destroyed. Upon excitation with light of a specific wavelength, a photosensitizer can produce reactive oxygen species (ROS) in the presence of molecular oxygen, thereby exhibiting a cytotoxic effect toward the surrounding tissues, giving a total control on the onset of therapy. In this research work, curcumin as a natural photosensitizer has been investigated against cancer cells. To enhance the solubility of curcumin, a nanoformulation is developed using chitosan as biodegradable and biocompatible polymer that has the ability to encapsulate curcumin and improve its therapeutic effect. Physicochemical characterizations revealed that the prepared formulations were in the nanoscale range and had a positive ζ‐potential. Upon irradiation using a novel LED device (λex = 457 nm), curcumin nanoparticles were able to generate ROS and destroy tumor cells. Moreover, unloaded nanoparticles exhibited nonsignificant phototoxicity. These outcomes confirm the importance of curcumin nanoparticles in enhancing the efficacy of curcumin and offer new insights in the field of PDT against cancer. [ABSTRACT FROM AUTHOR]