Keywords
therapy
liposomes
phosphatidylserine
antimony
nanoformulations
How to Cite
Abstract
Leishmaniasis is an endemic and tropical disease that afflicts mainly the developing countries. The limited and highly toxic therapeutic arsenal for leishmaniasis treatment still remains on antimony salts. The second line drugs as amphotericin B and pentamidine are also toxic, and no novel drug is available against Leishmania spp. Liposomes are effective drug delivery systems which can deliver high amounts of entrapped drugs to target cells. In this study, a strategic liposome formulation was developed in order to deliver the pentavalent antimony to Leishmania-infected macrophages through the in vivo interaction with scavenger receptors. Antimony-entrapped liposomes demonstrated a high efficacy in vivo reducing 133-fold the total antimony dose, with a 100% decrease in the liver parasite burden at 0.75 mg/kg dose. By transmission electron microscopy a stable formulation composed by oligolamellar vesicles with 0.2 μm was demonstrated. Zeta potential studies showed a negative charge attached to the external membrane of liposomes due to phosphatidylserine addition. This novel approach contributes to the study on novel liposomal formulations for reducing the toxic effects of drugs in Leishmaniasis therapy.References
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Copyright (c) 2008 Instituto Adolfo Lutz Journal
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