Photodynamic and photothermal therapies with IR780 have gained exponential interest, and their photophysical properties have demonstrated promise for use in antitumor and antimicrobial chemotherapy. IR780 and its derivatives are valuable in labeling nanostructures with different chemical compositions for in vitro and in vivo fluorescence monitoring studies in the near-infrared (NIR) spectrum. The current literature is abundant on this topic, particularly with applications in the treatment of different types of cancer using laser illumination to produce photodynamic (PDT), photothermal (PTT), and, more recently, sonodynamic therapy (SDT) approaches for cell death. This review aims to update the state of the art concerning IR780 photosensitizer as a theranostic agent for PDT, PTT, SDT, and photoacoustic (PA) effects, and fluorescence imaging monitoring associated with different types of nanocarriers. The literature update concerns a period from 2017 to 2024, considering, more specifically, the in vivo effects found in preclinical experiments. Some aspects of the labeling stability of nanostructured systems will be discussed based on the evidence of IR780 leakage from the nanocarrier and its consequences for the reliable analysis of biological data.

Standards of care for human visceral leishmaniasis (VL) are based on drugs used parenterally, and oral treatment options are urgently needed. In the present study, a repurposing strategy was used associating tamoxifen (TMX) with polyethylene glycol-block-polylactide nanocapsules (NC) and its anti-leishmanial efficacy was reported in vivo. Stable surface modified-NC (5 mg/mL of TMX) exhibited 200 nm in size, +42 mV of zeta potential, and 98% encapsulation efficiency. Atomic force microscopy evidenced core-shell-NC. Treatment with TMX-NC reduced parasite-DNA quantified in liver and spleen compared to free-TMX; and provided a similar reduction of parasite burden compared with meglumine antimoniate in mice and hamster models. Image-guided biodistribution showed accumulation of NC in liver and spleen after 30 min post-administration. TMX-NC reduced the number of liver granulomas and restored the aspect of capsules and trabeculae in the spleen of infected animals. TMX-NC was tested for the first time against VL models, indicating a promising formulation for oral treatment.