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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...

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Autores principales: Campos Vieira, N., Vacus, J., Fournet, A., Baudouin, R., Bories, C., Séon-Méniel, B., Figadère, B., Loiseau, P.M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: EDP Sciences 2011
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.
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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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