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

Pharmaceutics(2023)

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摘要
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 () 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 Sb 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 ( < 0.05) when compared to the untreated control group.
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关键词
acute toxicity,antileishmanial efficacy,emetic tartar,liposomes,visceral leishmaniasis
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