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Título: | Higher oral efficacy of ravuconazole in self-nanoemulsifying systems in shorter treatment in experimental chagas disease. |
Autor(es): | Spósito, Pollyanna Álvaro Mazzeti, Ana Lia Castro, Kelly Christyne Miranda Pereira de Mendes, Priscila Fagundes Urbina, Julio Alberto Bahia, Maria Terezinha Mosqueira, Vanessa Carla Furtado |
Palavras-chave: | Y strain Trypanosoma cruzi Ravuconazole Self-nanoemulsifying drug delivery system Efficacy |
Data do documento: | 2021 |
Referência: | SPÓSITO, P. A. et al. Higher oral efficacy of ravuconazole in self-nanoemulsifying systems in shorter treatment in experimental chagas disease. Experimental Parasitology, v. 228, artigo 108142, 2021. Disponível em: <https://www.sciencedirect.com/science/article/pii/S0014489421000795?via%3Dihub>. Acesso em: 11 out. 2022. |
Resumo: | We investigated the in vitro activity and selectivity, and in vivo efficacy of ravuconazole (RAV) in self- nanoemulsifying delivery system (SNEDDS) against Trypanosoma cruzi. Novel formulations of this poorly solu- ble C14-α-demethylase inhibitor may improve its efficacy in the experimental treatment. In vitro activity was determined in infected cardiomyocytes and efficacy in vivo evaluated in terms of parasitological cure induced in Y and Colombian strains of T. cruzi-infected mice. In vitro RAV-SNEDDS exhibited significantly higher potency of 1.9-fold at the IC50 level and 2-fold at IC90 level than free-RAV. No difference in activity with Colombian strain was observed in vitro. Oral treatment with a daily dose of 20 mg/kg for 30 days resulted in 70% of cure for RAV- SNEDDS versus 40% for free-RAV and 50% for 100 mg/kg benznidazole in acute infection (T. cruzi Y strain). Long-term treatment efficacy (40 days) was able to cure 100% of Y strain-infected animals with both RAV preparations. Longer treatment time was also efficient to increase the cure rate with benznidazole (Y and Colombian strains). RAV-SNEDDS shows greater efficacy in a shorter time treatment regimen, it is safe and could be a promising formulation to be evaluated in other pre-clinical models to treat T. cruzi and fungi infections. |
URI: | http://www.repositorio.ufop.br/jspui/handle/123456789/16511 |
Link para o artigo: | https://www.sciencedirect.com/science/article/pii/S0014489421000795?via%3Dihub |
DOI: | https://doi.org/10.1016/j.exppara.2021.108142 |
ISSN: | 0014-4894 |
Aparece nas coleções: | DECBI - Artigos publicados em periódicos |
Arquivos associados a este item:
Arquivo | Descrição | Tamanho | Formato | |
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ARTIGO_HigherOralEfficacy.pdf Restricted Access | 2 MB | Adobe PDF | Visualizar/Abrir |
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