Navegando por Autor "Andrade, Vinicius Roberto de"
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Item Repositioning of tamoxifen in surface-modified nanocapsules as a promising oral treatment for visceral leishmaniasis.(2021) Silva, Débora Faria; Reis, Levi Eduardo Soares; Machado, Marina Guimarães Carvalho; Dophine, Douglas Daniel; Andrade, Vinicius Roberto de; Lima, Wanderson Geraldo de; Andrade, Margareth Spangler; Vilela, José Mário Carneiro; Reis, Alexandre Barbosa; Lana, Gwenaelle Elza Nathalie Pound; Rezende, Simone Aparecida; Mosqueira, Vanessa Carla FurtadoStandards of care for human visceral leishmaniasis (VL) are based on drugs used parenter- ally, 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.