Pharmacokinetic of meglumine antimoniate encapsulated in phosphatidylserine-liposomes in mice model
| dc.contributor.author | BORBOREMA, SAMANTA E.T. | |
| dc.contributor.author | OSSO JUNIOR, JOAO A. | |
| dc.contributor.author | TEMPONE, ANDRE G. | |
| dc.contributor.author | ANDRADE JUNIOR, HEITOR F. de | |
| dc.contributor.author | NASCIMENTO, NANCI do | |
| dc.coverage | Internacional | pt_BR |
| dc.date.accessioned | 2018-11-26T10:42:26Z | |
| dc.date.available | 2018-11-26T10:42:26Z | |
| dc.date.issued | 2018 | pt_BR |
| dc.description.abstract | Visceral 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.sponsorship | Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) | pt_BR |
| dc.description.sponsorship | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) | pt_BR |
| dc.description.sponsorshipID | CNPq: 142839/2005-1; 201308/2008-8; 457099/2014-3 | pt_BR |
| dc.description.sponsorshipID | FAPESP: 14/24908-4 | pt_BR |
| dc.format.extent | 1609-1616 | pt_BR |
| dc.identifier.citation | BORBOREMA, 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.doi | 10.1016/j.biopha.2018.05.004 | pt_BR |
| dc.identifier.issn | 0753-3322 | pt_BR |
| dc.identifier.orcid | aguardando | pt_BR |
| dc.identifier.orcid | aguardando | pt_BR |
| dc.identifier.orcid | aguardando | pt_BR |
| dc.identifier.orcid | https://orcid.org/0000-0002-6672-1631 | |
| dc.identifier.percentilfi | 71.76 | pt_BR |
| dc.identifier.percentilfiCiteScore | 56.00 | |
| dc.identifier.uri | http://repositorio.ipen.br/handle/123456789/29275 | |
| dc.identifier.vol | 103 | pt_BR |
| dc.relation.ispartof | Biomedicine & Pharmacotherapy | pt_BR |
| dc.rights | openAccess | pt_BR |
| dc.subject | pharmacology | |
| dc.subject | radionuclide kinetics | |
| dc.subject | parasitic diseases | |
| dc.subject | liposomes | |
| dc.subject | antimony | |
| dc.subject | antimonates | |
| dc.subject | labelling | |
| dc.subject | toxicity | |
| dc.title | Pharmacokinetic of meglumine antimoniate encapsulated in phosphatidylserine-liposomes in mice model | pt_BR |
| dc.type | Artigo de periódico | pt_BR |
| dspace.entity.type | Publication | |
| ipen.autor | NANCI DO NASCIMENTO | |
| ipen.autor | JOAO ALBERTO OSSO JUNIOR | |
| ipen.autor | SAMANTA ETEL TREIGER BORBOREMA | |
| ipen.codigoautor | 411 | |
| ipen.codigoautor | 140 | |
| ipen.codigoautor | 3208 | |
| ipen.contributor.ipenauthor | NANCI DO NASCIMENTO | |
| ipen.contributor.ipenauthor | JOAO ALBERTO OSSO JUNIOR | |
| ipen.contributor.ipenauthor | SAMANTA ETEL TREIGER BORBOREMA | |
| ipen.date.recebimento | 18-11 | pt_BR |
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| ipen.identifier.fiCiteScore | 4.0 | |
| ipen.identifier.ipendoc | 25063 | pt_BR |
| ipen.identifier.iwos | WoS | pt_BR |
| ipen.range.fi | 3.000 - 4.499 | |
| ipen.range.percentilfi | 50.00 - 74.99 | |
| ipen.subtitulo | a candidate formulation for visceral leishmaniasis | pt_BR |
| ipen.type.genre | Artigo | |
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| sigepi.autor.atividade | BORBOREMA, SAMANTA E.T.:3208:-1:S | pt_BR |
| sigepi.autor.atividade | OSSO JUNIOR, JOAO A.:140:-1:N | pt_BR |
| sigepi.autor.atividade | NASCIMENTO, NANCI DO:411:-1:N | pt_BR |