Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model
| Autor: | Campos Vieira N., Vacus J., Fournet A., Baudouin R., Bories C., Séon-Méniel B., Figadère B., Loiseau P.M. |
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| Jazyk: | angličtina |
| Rok vydání: | 2011 |
| Předmět: | |
| Zdroj: | Parasite, Vol 18, Iss 4, Pp 333-336 (2011) |
| Druh dokumentu: | article |
| ISSN: | 1252-607X 1776-1042 20111843 |
| DOI: | 10.1051/parasite/2011184333 |
| Popis: | 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. |
| Databáze: | Directory of Open Access Journals |
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