Development of Nanoemulsions to Enhance the Antileishmanial Activity ofCopaifera pauperaOleoresins

Abstract

Based on the ethnopharmacological evidences about the antileishmanial activity ofCopaiferaspp. oleoresins, the effects of crude extracts and fractions of oleoresin of two specimens fromCopaifera pauperawere evaluated onLeishmania amazonensisandLeishmania infantumstrains. The oleoresin rich inα-copaene (38.8%) exhibited the best activity againstL. amazonensis(IC50= 62.5 μg/mL) and againstL. infantum(IC50= 65.9 μg/mL). The sesquiterpeneα-copaene isolated was tested alone and exhibited high antileishmanial activityin vitrowith IC50values forL. amazonensisandL. infantumof 17.2 and 11.4 μg/mL, respectively. In order to increase antileishmanial activity, nanoemulsions containing copaiba oleoresin andα-copaene were developed and assayed againstL. amazonensisandL. infantumpromastigotes. The nanoemulsion containingα-copaene (NANOCOPAEN) showed the best activity against both species, with IC50of 2.5 and 2.2 μg/mL, respectively. This is the first report about the antileishmanial activity ofα-copaene.