| Author | Spósito, Pollyanna Álvaro | |
| Author | Mazzeti, Ana Lia | |
| Author | Castro, Kelly Christyne Miranda Pereira de | |
| Author | Mendes, Priscila Fagundes | |
| Author | Urbina, Julio A. | |
| Author | Bahia, Maria Terezinha | |
| Author | Mosqueira, Vanessa Carla Furtado | |
| Access date | 2021-12-03T11:51:11Z | |
| Available date | 2021-12-03T11:51:11Z | |
| Document date | 2021 | |
| Citation | SPÓSITO, Pollyanna Álvaro et al. Higher oral efficacy of ravuconazole in self-nanoemulsifying systems in shorter treatment in experimental chagas disease. Experimental Parasitology, v. 228, 108142, p. 1 - 8, 2021. | pt_BR |
| ISSN | 0014-4894 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/50137 | |
| Language | eng | pt_BR |
| Publisher | Elsevier | pt_BR |
| Rights | restricted access | |
| Subject in Portuguese | Trypanosoma cruzi | pt_BR |
| Subject in Portuguese | Ravuconazol | pt_BR |
| Subject in Portuguese | Sistema de administração de drogas autonanoemulsificantes | pt_BR |
| Subject in Portuguese | Eficácia | pt_BR |
| Subject in Portuguese | Toxicidade | pt_BR |
| Subject in Portuguese | Linhagem colombiana | pt_BR |
| Subject in Portuguese | Cepa Y | pt_BR |
| Title | Higher oral efficacy of ravuconazole in self-nanoemulsifying systems in shorter treatment in experimental chagas disease | pt_BR |
| Type | Article | |
| DOI | 10.1016/j.exppara.2021.108142 | |
| Abstract | We investigated the in vitro activity and selectivity, and in vivo efficacy of ravuconazole (RAV) in selfnanoemulsifying
delivery system (SNEDDS) against Trypanosoma cruzi. Novel formulations of this poorly soluble
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 RAVSNEDDS
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. | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Escola de Farmácia. Laboratório de Farmacêutica e Nanotecnologia. Ouro Preto, MG, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Escola de Farmácia. Laboratório de Farmacêutica e Nanotecnologia. Ouro Preto, MG, Brasil / Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Escola de Farmácia. Laboratório de Farmacêutica e Nanotecnologia. Ouro Preto, MG, Brasil / Universidade Federal de Ouro Preto. Escola de Medicina. Laboratório de Doenças Parasitárias. Ouro Preto, MG, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Escola de Farmácia. Laboratório de Farmacêutica e Nanotecnologia. Ouro Preto, MG, Brasil. | pt_BR |
| Affilliation | Venezuelan Institute for Scientific Research, Caracas, 1020A, Venezuela. | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Escola de Medicina. Laboratório de Doenças Parasitárias. Ouro Preto, MG, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Ouro Preto. Escola de Farmácia. Laboratório de Farmacêutica e Nanotecnologia. Ouro Preto, MG, Brasil. | pt_BR |
| Subject | Trypanosoma cruzi | pt_BR |
| Subject | Ravuconazole | pt_BR |
| Subject | Self-nanoemulsifying drug delivery system | pt_BR |
| Subject | Efficacy | pt_BR |
| Subject | Toxicity | pt_BR |
| Subject | Colombian strain | pt_BR |
| Subject | Y strain | pt_BR |
| Embargo date | 2023 | |
