BORBOREMA, SAMANTA E.T.OSSO JUNIOR, JOAO A.TEMPONE, ANDRE G.ANDRADE JUNIOR, HEITOR F. deNASCIMENTO, NANCI do2018-11-262018-11-262018BORBOREMA, SAMANTA E.T.; OSSO JUNIOR, JOAO A.; TEMPONE, ANDRE G.; ANDRADE JUNIOR, HEITOR F. de; NASCIMENTO, NANCI do. Pharmacokinetic of meglumine antimoniate encapsulated in phosphatidylserine-liposomes in mice model: a candidate formulation for visceral leishmaniasis. <b>Biomedicine & Pharmacotherapy</b>, v. 103, p. 1609-1616, 2018. DOI: <a href="https://dx.doi.org/10.1016/j.biopha.2018.05.004">10.1016/j.biopha.2018.05.004</a>. Disponível em: http://repositorio.ipen.br/handle/123456789/29275.0753-3322http://repositorio.ipen.br/handle/123456789/29275Visceral leishmaniasis (VL) is a fatal parasitic disease caused by the protozoan Leishmania spp. Meglumine antimoniate (MA) is the main treatment and has demonstrated a promising efficacy in a VL-model when encapsulated into negatively charged liposomes. Considering the current concept for the evaluation of pharmacokinetic parameters at early phases of drug discovery, we developed a formulation of MA-encapsulated into phosphatidylserine liposomes (MA-LP) and analyzed the in vitro antileishmanial activity, physicochemical properties, and pharmacokinetic profile in a mice model. The liposomal formulation had an internal mean diameter of 114 nm and a high stability in plasma. MA-LP was 23-fold more in vitro effective against Leishmania infantum-infected macrophages than the free drug, with a selectivity index higher than 220. The pharmacokinetic studies demonstrated that the liposomes increased the uptake of the drug by the liver and spleen and promoted sustained levels. MA-LP was first eliminated through renal excretion, followed by biliary excretion. In the blood, MA-LP followed a biexponential open model. This work emphasizes the importance of liposomes as potential drug delivery systems for visceral leishmaniasis.1609-1616openAccesspharmacologyradionuclide kineticsparasitic diseasesliposomesantimonyantimonateslabellingtoxicityArtigo de periódico10310.1016/j.biopha.2018.05.004aguardandoaguardandoaguardandohttps://orcid.org/0000-0002-6672-163171.7656.00