Full metadata record
DC Field | Value | Language |
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dc.creator | Etxebeste-Mitxeltorena, M. (Mikel) | - |
dc.creator | Moreno-Amatria, E. (Esther) | - |
dc.creator | Carvalheiro, M. (Manuela) | - |
dc.creator | Calvo-Bacaicoa, A. (Alba) | - |
dc.creator | Navarro-Blasco, I. (Iñigo) | - |
dc.creator | Gonzalez-Peñas, E. (Elena) | - |
dc.creator | Alvarez-Galindo, J.I. (José Ignacio) | - |
dc.creator | Plano-Amatriain, D. (Daniel) | - |
dc.creator | Irache, J.M. (Juan Manuel) | - |
dc.creator | Almeida, A.J. (Antonio J.) | - |
dc.creator | Sanmartin-Grijalba, C. (Carmen) | - |
dc.creator | Espuelas, S. (Socorro) | - |
dc.date.accessioned | 2022-02-18T11:03:23Z | - |
dc.date.available | 2022-02-18T11:03:23Z | - |
dc.date.issued | 2021 | - |
dc.identifier.citation | Etxebeste-Mitxeltorena, M. (Mikel); Moreno-Amatria, E. (Esther); Carvalheiro, M.; et al. "Oral efficacy of a diselenide compound loaded in nanostructured lipid carriers in a murine model of visceral leishmaniasis". ACS Infectious Diseases. 7 (12), 2021, 3197 - 3209 | es |
dc.identifier.issn | 2373-8227 | - |
dc.identifier.uri | https://hdl.handle.net/10171/62944 | - |
dc.description.abstract | Leishmaniasis urgently needs new oral treatments, as it is one of the most important neglected tropical diseases that affects people with poor resources. The drug discovery pipeline for oral administration currently discards entities with poor aqueous solubility and permeability (class IV compounds in the Biopharmaceutical Classification System, BCS) such as the diselenide 2m, a trypanothione reductase (TR) inhibitor. This work was assisted by glyceryl palmitostearate and diethylene glycol monoethyl ether-based nanostructured lipid carriers (NLC) to render 2m bioavailable and effective after its oral administration. The loading of 2m in NLC drastically enhanced its intestinal permeability and provided plasmatic levels higher than its effective concentration (IC50). In L. infantum-infected BALB/c mice, 2m-NLC reduced the parasite burden in the spleen, liver, and bone marrow by at least 95% after 5 doses, demonstrating similar efficacy as intravenous Fungizone. Overall, compound 2m and its formulation merit further investigation as an oral treatment for visceral leishmaniasis. | - |
dc.description.sponsorship | Mikel Etxebeste Miltxetorena received a grant from the The Institute of Tropical Health (ISTUN, University of Navarra). The work was supported by The Institute of Tropical Health (ISTUN, University of Navarra) and funders (Obra Social La Caixa and Fundación Caja Navarra, Fundación Roviralta, PROFAND, Ubesol, ACUNSA, and Artai) | - |
dc.language.iso | en | - |
dc.rights | info:eu-repo/semantics/openAccess | - |
dc.subject | Diselenide | - |
dc.subject | Nanostructured lipid carriers | - |
dc.subject | Visceral leishmanisis | - |
dc.subject | L. infantum | - |
dc.subject | Oral treatment | - |
dc.title | Oral efficacy of a diselenide compound loaded in nanostructured lipid carriers in a murine model of visceral leishmaniasis | - |
dc.type | info:eu-repo/semantics/article | - |
dc.description.note | CC BY | - |
dc.identifier.doi | 10.1021/acsinfecdis.1c00394 | - |
dadun.citation.endingPage | 3209 | - |
dadun.citation.number | 12 | - |
dadun.citation.publicationName | ACS Infectious Diseases | - |
dadun.citation.startingPage | 3197 | - |
dadun.citation.volume | 7 | - |
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