In vitro effect of artemether-loaded nanostructured lipid carrier (NLC) on Leishmania infantum

Abstract

Visceral leishmaniasis (VL) is an acute and deadly form of leishmaniasis, caused by Leishmania infantum parasite. Due to the toxicity and side effects of conventional treatment options, such as glucantime and other pentavalent drugs, finding novel drugs with fewer adverse effects is required. Artemether (ART), is one of the derivatives of artemisinin, which was shown to be effective in treating malaria and more recently, leishmaniasis. In this fundamental-applied research, we compared the effect of ART and nanostructure loaded with artemether (NLC-ART) on Leishmania infantum promastigotes and amastigotes, at different concentrations (2.5-5-10-25-50-100 μg/ml) using the MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay method after 24 and 48 h of treatment. Inhibitory concentration (IC50) values (μg/ml) of promastigote and amastigote of L. infantum to ART/ NLC-ART, after 48 h of treatment, were found to be 37.12 / 32.1 and 16.43 / 15.42, respectively. Moreover, we found that (NLC-ART), had the lowest cytotoxicity against the J774 macrophage cell line. Conclusion: The NLC-ART can be a good candidate for the treatment of visceral leishmaniasis.

Keywords: Artemether; Drug delivery; Leishmania infantum; MTT assay; Nanostructured lipid carrier (NLC).

Fig. 1

Viability of the L. infantum promastigotes after 24 h at different concentrations of the formulations

Fig. 2

Viability of the L. infantum promastigotes after 48 h at different concentrations of the formulations

Fig. 3

Parasite burden after 24 h at different concentrations of the formulations

Fig. 4

Parasite burden after 48 h at different concentrations of the formulations

Fig. 5

Evaluation of cytotoxicity of various formulations on J774 cells after 24 h. Amphotericin B is positive control

Fig. 6

Evaluation of cytotoxicity of various formulations on J774 cells after 48 h. Amphotericin B is positive control