| Author | Damasio, Danielle Sóter do Nascimento | |
| Author | Antunes, Patrícia Andrade | |
| Author | Lages, Eduardo Burgarelli | |
| Author | Teixeira, Eliane de Morais | |
| Author | Vital, Kátia Duarte | |
| Author | Cardoso, Valbert Nascimento | |
| Author | Fernandes, Simone Odılia Antunes | |
| Author | Aguiar, Marta Gontijo | |
| Author | Ferreira, Lucas Antônio Miranda | |
| Access date | 2023-01-27T19:12:02Z | |
| Available date | 2023-01-27T19:12:02Z | |
| Document date | 2022 | |
| Citation | DO NASCIMENTO DAMASIO, Danielle Sóter et al. A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo. International Journal of Pharmaceutics, 122505, 2022. Doi: 10.1016/j.ijpharm.2022.122505 | en_US |
| ISSN | 0378-5173 | en_US |
| URI | https://www.arca.fiocruz.br/handle/icict/56714 | |
| Language | eng | en_US |
| Publisher | Elsevier/North-Holland Biomedical Press | en_US |
| Rights | restricted access | |
| Title | A new oral self-emulsifying drug delivery system improves the antileishmania efficacy of fexinidazole in vivo | en_US |
| Type | Article | |
| Abstract | The aim of this study was to develop, characterize and evaluate the in vivo oral efficacy of self-emulsifying drug delivery systems (SEDDS) containing fexinidazole (FEX) in the experimental treatment of visceral leishmaniasis (VL). The developed FEX-SEDDS formulation presented as a clear, yellowish liquid, with absence of precipitate. The droplet size, polydispersion index and zeta potential after dilution in water (1:200) was of 91 ± 3 nm, 0.242 ± 0.005 and -16.7 ± 0.2, respectively. In the simulated gastric and intestinal media, the FEX-SEDDS had a size of 97 ± 1 and 106 ± 9 nm, respectively. The FEX retention in droplet after SEDDS dilution in simulated gastrointestinal media was almost 100 %. Antileishmanial efficacy studies showed that FEX-SEDDS was the only treatment able to significantly (p < 0.05) reduce the parasite burden in the liver and spleen of animals experimentally infected with Leishmania infantum. Our intestinal permeability data suggest that FEX-SEDDS showed no evidence of injury to the intestinal mucosa. These findings suggest that FEX-SEDDS can be a promising oral alternative for the treatment of VL caused by L. infantum. | en_US |
| Affilliation | Department of Pharmaceutical Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil. | en_US |
| Affilliation | Department of Pharmaceutical Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil. | en_US |
| Affilliation | Department of Pharmaceutical Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil. | en_US |
| Affilliation | Clinical Research and Public Policy Group on Infectious and Parasitic Diseases. René Rachou Institute. Oswaldo Cruz Foundation. Belo Horizonte, MG, Brazil. | en_US |
| Affilliation | Department of Clinical and Toxicological Analysis. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil. | en_US |
| Affilliation | Department of Clinical and Toxicological Analysis. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil. | en_US |
| Affilliation | Department of Clinical and Toxicological Analysis. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil. | en_US |
| Affilliation | Department of Pharmaceutical Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil. | en_US |
| Affilliation | Department of Pharmaceutical Sciences. Federal University of Minas Gerais. Belo Horizonte, MG, Brazil. | en_US |
| Subject | Fexinidazole | en_US |
| Subject | Intestinal permeability | en_US |
| Subject | Oral treatment | en_US |
| Subject | Self-emulsifying drug release system | en_US |
| Subject | Visceral leishmaniasis | en_US |
| Embargo date | 2099-12-31 | |
