Efficacy of topical Miltefosine formulations in an experimental model of cutaneous leishmaniasis

PERALTA, MA. FLORENCIA; USSEGLIO, NADINA A.; BRACAMONTE, MA. ESTEFANÍA; GUZMÁN, MA. LAURA; OLIVERA, MA. EUGENIA; MARCO, J. DIEGO; BARROSO, PAOLA A.; CARRER, DOLORES C.

Drug Delivery and Translational Research

Springer

Año: 2021

2190-393X

utaneous leishmaniasis (CL) is a neglected tropical disease endemic in ~ 90 countries, with an increasing incidence. Presently available pharmacotherapy implies the systemic administration of moderately/very toxic drugs. Miltefosine (Milt) is the only FDA-approved drug to treat CL via the oral route (Impavido®). It produces side effects; in particular, teratogenic effects are of concern. A topical treatment would have the great advantage of minimising the systemic circulation of the drug, preventing side effects. We prepared dispersions containing Milt and liposomes of different compositions to enhance/modulate trans-epidermal penetration and evaluated in vitro and in vivo efficacy and toxicity, in vitro release rate of the drug and particles size stability with time. Treatments were topically administered to BALB/c mice infected with Leishmania (Leishmania) amazonensis. The dispersions containing 0.5% Milt eliminated 99% of the parasites and cured the lesions with a complete re-