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

Carregando...
Imagem de Miniatura
Data
2018
Data de publicação:
Orientador
Título da Revista
ISSN da Revista
Título do Volume
É parte de
É parte de
É parte de
Biomedicine & Pharmacotherapy
Exportar
Mendeley
Projetos de Pesquisa
Unidades Organizacionais
Fascículo
Resumo
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.

Como referenciar
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. Biomedicine & Pharmacotherapy, v. 103, p. 1609-1616, 2018. DOI: 10.1016/j.biopha.2018.05.004. Disponível em: http://repositorio.ipen.br/handle/123456789/29275. Acesso em: 28 Mar 2024.
Esta referência é gerada automaticamente de acordo com as normas do estilo IPEN/SP (ABNT NBR 6023) e recomenda-se uma verificação final e ajustes caso necessário.

Agência de fomento
Coleções