Abstract
Background: Leishmaniasis is a zoonotic disease caused by protozoan parasites from Leishmania genus. Currently, there are no effective vaccines available and the available therapies are far from ideal. In particular, the development of new therapeutic strategies to reduce the infection caused by Leishmania amazonensis could be considered desirable. Different plant-derived products have demonstrated antileishmanial activity, including the essential oil (EO) from Artemisia absinthium L. (EO-Aa), Asteraceae. Methods: In the present study, the EO-Aa formulated in nanocochleates (EO-Aa-NC) was investigated in vitro against intracellular amastigotes of L. amazonensis and non-infected macrophages from BALB/c mice. In addition, the EO-Aa-NC was also evaluated in vivo against on experimental cutaneous leishmaniasis, which body weight, lesion progression, and parasite load were determined. Results: EO-Aa-NC displayed IC50 values of 21.5 ± 2.5 μg/mL and 27.7 ± 5.6 μg/mL against intracellular amastigotes of L. amazonensis and non-infected peritoneal macrophage, respectively. In the animal model, the EO-Aa-NC (30 mg/kg/intralesional route/every 4 days 4 times) showed no deaths or weight loss greater than 10%. In parallel, the EO-Aa-NC suppressed the infection in the murine model by approximately 50%, which was statistically superior (p < 0.05) than controls and mice treated with EO-Aa. In comparison with Glucantime®, EO-Aa-NC inhibited the progression of infection as efficiently (p > 0.05) as administration of the reference drug. Conclusions: Encochleation of EO-Aa resulted in a stable, tolerable, and efficacious antileishmanial formulation, facilitating systemic delivery of EO, with increased activity compared to administration of the free EO-Aa. This new formulation shows promising potential to future studies aimed at a new therapeutic strategy to treat leishmaniasis.
Highlights
Leishmaniasis is a zoonotic disease caused by protozoan parasites from Leishmania genus (Trypanosomatidae), which is a transmitted by the bites of infected female sandflies
Encochleation of essential oil (EO)-Aa resulted in a stable, tolerable, and efficacious antileishmanial formulation, facilitating systemic delivery of EO, with increased activity compared to administration of the free EO-Aa
The purpose of the present study was to investigate the effect of essential oil from A. absinthium formulated in nanocochleate against L. amazonensis, including in vitro assays and in vivo models
Summary
Leishmaniasis is a zoonotic disease caused by protozoan parasites from Leishmania genus (Trypanosomatidae), which is a transmitted by the bites of infected female sandflies. Over 20 species of protozoan have been reported as pathogenic to humans [1]. This obligate intracellular parasite has a complex digenetic life cycle, which requires a susceptible vertebrate host, as well as Medicines 2017, 4, 38; doi:10.3390/medicines4020038 www.mdpi.com/journal/medicines. There are no effective vaccines currently available for any form of leishmaniasis, while the available therapies are far from ideal due to their toxicity, high costs, lack of efficacy, difficult access in certain areas, and emerging drug resistance [6]. Leishmaniasis is a zoonotic disease caused by protozoan parasites from.
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