Therapeutic evaluation of activatable melittin for selective treatment of leishmaniasis in vitro and in vivo

Abstract

Leishmaniasis is a major public health problem worldwide. Because of its high prevalence, the development of an effective treatment is especially important. Drug delivery systems are promising pharmaceutical formulations for improving the therapeutic index of drugs. In this study, activatable melittin (AM) peptide was designed and encapsulated with albumin and liposome for selective targeting of Leishmania infected cells. The effect of AM was determined by measuring its cytotoxicity and pathologic effects using Giemsa and haematoxylin/eosin staining, respectively. The results of this study showed that the toxicity of designed AM is reduced compared to wild-type melittin, in addition to the use of AM-loaded albumin nanoparticle and liposome containing AM and their therapeutic role against cutaneous leishmaniasis caused by L. major. The encapsulation of AM with albumin and liposome as a non-toxic carrier at a concentration of 25 µg/mL can improve and optimise the antileishmanial effects of this drug, so, infected cells treated with AM in albumin nanoparticle and liposome had less Leishmania major promastigotes. These forms of the drug could be a good alternative to the current drugs so performance of further in vivo studies is suggested.

Keywords

• activatable melittin
• balb/c mice
• cutaneous leishmaniasis