Pharmacokinetic of meglumine antimoniate encapsulated in phosphatidylserine-liposomes in mice model

dc.contributor.authorBORBOREMA, SAMANTA E.T.
dc.contributor.authorOSSO JUNIOR, JOAO A.
dc.contributor.authorTEMPONE, ANDRE G.
dc.contributor.authorANDRADE JUNIOR, HEITOR F. de
dc.contributor.authorNASCIMENTO, NANCI do
dc.coverageInternacionalpt_BR
dc.date.accessioned2018-11-26T10:42:26Z
dc.date.available2018-11-26T10:42:26Z
dc.date.issued2018pt_BR
dc.description.abstractVisceral 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.pt_BR
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)pt_BR
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)pt_BR
dc.description.sponsorshipIDCNPq: 142839/2005-1; 201308/2008-8; 457099/2014-3pt_BR
dc.description.sponsorshipIDFAPESP: 14/24908-4pt_BR
dc.format.extent1609-1616pt_BR
dc.identifier.citationBORBOREMA, 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.
dc.identifier.doi10.1016/j.biopha.2018.05.004pt_BR
dc.identifier.issn0753-3322pt_BR
dc.identifier.orcidaguardandopt_BR
dc.identifier.orcidaguardandopt_BR
dc.identifier.orcidaguardandopt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-6672-1631
dc.identifier.percentilfi71.76pt_BR
dc.identifier.percentilfiCiteScore56.00
dc.identifier.urihttp://repositorio.ipen.br/handle/123456789/29275
dc.identifier.vol103pt_BR
dc.relation.ispartofBiomedicine & Pharmacotherapypt_BR
dc.rightsopenAccesspt_BR
dc.subjectpharmacology
dc.subjectradionuclide kinetics
dc.subjectparasitic diseases
dc.subjectliposomes
dc.subjectantimony
dc.subjectantimonates
dc.subjectlabelling
dc.subjecttoxicity
dc.titlePharmacokinetic of meglumine antimoniate encapsulated in phosphatidylserine-liposomes in mice modelpt_BR
dc.typeArtigo de periódicopt_BR
dspace.entity.typePublication
ipen.autorNANCI DO NASCIMENTO
ipen.autorJOAO ALBERTO OSSO JUNIOR
ipen.autorSAMANTA ETEL TREIGER BORBOREMA
ipen.codigoautor411
ipen.codigoautor140
ipen.codigoautor3208
ipen.contributor.ipenauthorNANCI DO NASCIMENTO
ipen.contributor.ipenauthorJOAO ALBERTO OSSO JUNIOR
ipen.contributor.ipenauthorSAMANTA ETEL TREIGER BORBOREMA
ipen.date.recebimento18-11pt_BR
ipen.identifier.fi3.743pt_BR
ipen.identifier.fiCiteScore4.0
ipen.identifier.ipendoc25063pt_BR
ipen.identifier.iwosWoSpt_BR
ipen.range.fi3.000 - 4.499
ipen.range.percentilfi50.00 - 74.99
ipen.subtituloa candidate formulation for visceral leishmaniasispt_BR
ipen.type.genreArtigo
relation.isAuthorOfPublication53eed426-0bd7-4230-8b8c-f48795fad345
relation.isAuthorOfPublicationb0d5c854-8fcb-4e5f-b1c9-73e82c9ca844
relation.isAuthorOfPublication1dfe7126-d43b-4783-8093-9a1db0e81f97
relation.isAuthorOfPublication.latestForDiscovery1dfe7126-d43b-4783-8093-9a1db0e81f97
sigepi.autor.atividadeBORBOREMA, SAMANTA E.T.:3208:-1:Spt_BR
sigepi.autor.atividadeOSSO JUNIOR, JOAO A.:140:-1:Npt_BR
sigepi.autor.atividadeNASCIMENTO, NANCI DO:411:-1:Npt_BR

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