ANTILEISHMANIAL ACTIVITY OF A FORMULATION OF 2-N-PROPYLQUINOLINE BY ORAL ROUTE IN MICE MODEL

作者：Vieira Campos N; Vacus J; Fournet A; Baudouin R; Bories C; Seon Meniel B; Figadere B; Loiseau P M^*

来源：Parasite, 2011, 18(4): 333-336.

• leishmaniosis
• quinoline
• antileishmanial
• drug formulation

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 mu moles/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.

• 出版日期2011-11