Polymeric micelle loaded with lapachol for topical treatment of mice infected with Leishmania (Leishmania) major.

Cutaneous leishmaniasis (CL) is a neglected tropical disease. The treatment is restricted to a handful number of drugs that exhibit toxic effects and limited efficacy. The development of new alternative therapies, including the identification of effective drugs for topical treatment of CL, is of utmost interest. The aim of this study was to prepare, characterize and evaluate the efficacy of topical therapy with lapachol-micelle in the experimental treatment of CL. The lapachol-micelle was prepared using polaxamer 407. A preliminary stability study was conducted for 15 days at room temperature. The antileishmanial efficacy was performed in BALB/c mice infected with Leishmania (Leishmania) major, the treatment groups were: topical lapachol-micelle, intraperitoneal Glucantime, and control (untreated). Therapeutic efficacy was assessed by parasite load, and lesion size. To evaluate toxicity, the animals were weighed and blood was collected for biochemical analysis. Lapachol-micelle presented adequate characteristics: size 15 nm, zeta potential -3mV, and polydispersity index 0.3; remaining stable in preliminary stability study. Treatment with lapachol-micelle resulted in significant improvement, leading to stabilization of lesion size, while in the other groups, lesions increased in size. No significant changes were observed in weight or biochemical parameters. Topical treatment with lapachol-micelle may be a promising alternative for the treatment of CL.