Pharmaceutics (Mar 2023)

Emetic Tartar-Loaded Liposomes as a New Strategy for Leishmaniasis Treatment

  • Larissa D. Coelho,
  • Mirna M. D. Souza,
  • Geovanni D. Cassali,
  • Raphaela A. Silva,
  • Maria J. N. Paiva,
  • André L. B. Barros,
  • Eliane M. Teixeira,
  • Josianne N. Silveira,
  • Paulo M. Z. Coelho,
  • Marta M. G. Aguiar,
  • Mônica C. Oliveira

DOI
https://doi.org/10.3390/pharmaceutics15030904
Journal volume & issue
Vol. 15, no. 3
p. 904

Abstract

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Emetic tartar (ET), was used in the treatment of leishmaniasis but its use was discontinued due to its low therapeutic index. Liposomes have been shown to be a promising strategy for delivery of bioactive substances in the region of interest, in order to reduce and/or eliminate undesirable effects. In the present study, liposomes containing ET were prepared and characterized to evaluate acute toxicity as well as their leishmanicidal action using BALB/c mice with an inoculum of Leishmania (Leishmania) infantum. Liposomes were composed of egg phosphatidylcholine and 3ß-[N-(N′,N′-dimethylaminoethane)-carbamoyl]cholesterol, with an average diameter of 200 nm, zeta potential of +18 mV, and ET encapsulated into liposomes at a concentration near 2 g/L. Healthy mice were treated with ET or liposome containing ET (Lip-ET) in a single dose of 16 mg/kg of Sb3+ intravenously and observed for 14 days. The death of two animals in the ET-treated group and no deaths in the Lip-ET-treated group was observed. Higher hepatic and cardiac toxicity were observed in animals treated with ET when compared to animals treated with Lip-ET, blank liposomes (Blank-Lip) and PBS. The study of antileishmanial efficacy was conducted by intraperitoneal administration of Lip-ET, for ten consecutive days. It was observed by limiting dilution that treatments with liposomal formulations containing ET, as well as Glucantime®, led to a significant reduction in parasitic load in spleen and liver (p < 0.05) when compared to the untreated control group.

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