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Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model
2-n-propylquinoline is presently a drug-candidate for the treatment of visceral leishmaniosis in pre-clinical development. As this compound is in an oily state, it needs to be formulated and the objectives of this study are: to prepare a formulation; to demonstrate that the new salted formulation di...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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EDP Sciences
2011
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3677589/ https://www.ncbi.nlm.nih.gov/pubmed/22091464 http://dx.doi.org/10.1051/parasite/2011184333 |
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author | Campos Vieira, N. Vacus, J. Fournet, A. Baudouin, R. Bories, C. Séon-Méniel, B. Figadère, B. Loiseau, P.M. |
author_facet | Campos Vieira, N. Vacus, J. Fournet, A. Baudouin, R. Bories, C. Séon-Méniel, B. Figadère, B. Loiseau, P.M. |
author_sort | Campos Vieira, N. |
collection | PubMed |
description | 2-n-propylquinoline is presently a drug-candidate for the treatment of visceral leishmaniosis in pre-clinical development. As this compound is in an oily state, it needs to be formulated and the objectives of this study are: to prepare a formulation; to demonstrate that the new salted formulation did not alter the activity of the active ingredient; and finally, that this activity was quite good compared to the reference oral drug, miltefosine. Therefore, a 2-n-propylquinoline formulation, as camphorsulfonic salt, was prepared and characterised. On the Leishmania donovani / Balb/c mice model, a treatment by oral route at 60 μmoles/kg/day for ten consecutive days with this formulation was compared to 2-n-propylquinoline alone and to miltefosine, the oral reference drug. The salt formulation did not alter the activity of the 2-n-propylquinoline. The formulation reduced the parasite burden of 76% compared to 89% for miltefosine (not significant). The characteristics of this formulation results in a suitable drugability of 2-n-propylquinoline for further studies. |
format | Online Article Text |
id | pubmed-3677589 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | EDP Sciences |
record_format | MEDLINE/PubMed |
spelling | pubmed-36775892013-07-24 Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model Campos Vieira, N. Vacus, J. Fournet, A. Baudouin, R. Bories, C. Séon-Méniel, B. Figadère, B. Loiseau, P.M. Parasite Research Note 2-n-propylquinoline is presently a drug-candidate for the treatment of visceral leishmaniosis in pre-clinical development. As this compound is in an oily state, it needs to be formulated and the objectives of this study are: to prepare a formulation; to demonstrate that the new salted formulation did not alter the activity of the active ingredient; and finally, that this activity was quite good compared to the reference oral drug, miltefosine. Therefore, a 2-n-propylquinoline formulation, as camphorsulfonic salt, was prepared and characterised. On the Leishmania donovani / Balb/c mice model, a treatment by oral route at 60 μmoles/kg/day for ten consecutive days with this formulation was compared to 2-n-propylquinoline alone and to miltefosine, the oral reference drug. The salt formulation did not alter the activity of the 2-n-propylquinoline. The formulation reduced the parasite burden of 76% compared to 89% for miltefosine (not significant). The characteristics of this formulation results in a suitable drugability of 2-n-propylquinoline for further studies. EDP Sciences 2011-11 2011-11-15 /pmc/articles/PMC3677589/ /pubmed/22091464 http://dx.doi.org/10.1051/parasite/2011184333 Text en © PRINCEPS Editions, Paris, 2011 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Note Campos Vieira, N. Vacus, J. Fournet, A. Baudouin, R. Bories, C. Séon-Méniel, B. Figadère, B. Loiseau, P.M. Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model |
title | Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model |
title_full | Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model |
title_fullStr | Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model |
title_full_unstemmed | Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model |
title_short | Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model |
title_sort | antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model |
topic | Research Note |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3677589/ https://www.ncbi.nlm.nih.gov/pubmed/22091464 http://dx.doi.org/10.1051/parasite/2011184333 |
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