title: Antileishmanial activity of a formulation of 2-n-propylquinoline by oral route in mice model.
abstract: 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 mmoles/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.
authors.affiliation: Groupe Chimiothérapie Antiparasitaire, UMR 8076 CNRS, Faculté de Pharmacie, Université Paris-Sud, Rue Jean-Baptiste, 92296 Châtenay-Malabry Cedex, France.
authors.forename: N
authors.initials: N
authors.lastname: Campos Vieira
authors.forename: J
authors.initials: J
authors.lastname: Vacus
authors.forename: A
authors.initials: A
authors.lastname: Fournet
authors.forename: R
authors.initials: R
authors.lastname: Baudouin
authors.forename: C
authors.initials: C
authors.lastname: Bories
authors.forename: B
authors.initials: B
authors.lastname: Séon-Méniel
authors.forename: B
authors.initials: B
authors.lastname: Figadère
authors.forename: P M
authors.initials: PM
authors.lastname: Loiseau
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000981:Antiprotozoal Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical; D004195:Disease Models, Animal; D007893:Leishmania donovani / Q000187:drug effects*; D007898:Leishmaniasis, Visceral / Q000188:drug therapy*; D051379:Mice; D008807:Mice, Inbred BALB C; D010767:Phosphorylcholine / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000494:pharmacology; D011804:Quinolines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C116019:2-propylquinoline; D000981:Antiprotozoal Agents; D011804:Quinolines; D010767:Phosphorylcholine; C039128:miltefosine
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