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| Borborema,Samanta Etel Treiger; Andrade Junior,Heitor Franco de; Osso Junior,João Alberto; Nascimento,Nanci do. |
| Pentavalent antimony, as meglumine antimoniate (Glucantime® ) or sodium stibogluconate (Pentostam® ), is the main treatment for leishmaniasis, a complex of diseases caused by the protozoan Leishmania, and an endemic and neglected threat in Brazil. Despite over half a century of clinical use, their mechanism of action, toxicity and pharmacokinetic data remain unknown. The analytical methods for determination of antimony in biological systems remain complex and have low sensitivity. Radiotracer studies have a potential in pharmaceutical development. The aim of this study was to obtain a radiotracer for antimony, with suitable physical and biological properties. Meglumine antimoniate was neutron irradiated inside the IEA-R1 nuclear reactor, producing two... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Meglumine antimoniate; Leishmaniasis; Leishmania (L.) chagasi; Radiotracer. |
| Ano: 2005 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1516-89132005000700009 |
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| Schettini,D.A.; Costa Val,A.P.; Souza,L.F.; Demicheli,C.; Rocha,O.G.F.; Melo,M.N.; Michalick,M.S.M.; Frézard,F.. |
| The achievement of complete cure in dogs with visceral leishmaniasis is currently a great challenge, since dogs are the main reservoir for the transmission of visceral leishmaniasis to humans and they respond poorly to conventional treatment with pentavalent antimonials. In order to improve the efficacy of treatment, we developed a novel formulation for meglumine antimoniate based on the encapsulation of this drug in freeze-dried liposomes (LMA). The aim of the present study was to evaluate the biodistribution of antimony (Sb) in dogs following a single intravenous bolus injection of LMA. Four healthy male mongrel dogs received LMA at 3.8 mg Sb/kg body weight and were sacrificed 3, 48 and 96 h and 7 days later. Antimony was determined in the blood, liver,... |
| Tipo: Info:eu-repo/semantics/other |
Palavras-chave: Liposomes; Meglumine antimoniate; Biodistribution; Leishmaniasis; Dogs. |
| Ano: 2003 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2003000200015 |
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| Schettini,D.A.; Costa Val,A.P.; Souza,L.F.; Demicheli,C.; Rocha,O.G.F.; Melo,M.N.; Michalick,M.S.M.; Frézard,F.. |
| The aim of the present study was to evaluate the impact of a multiple dose regimen of a liposomal formulation of meglumine antimoniate (LMA) on the pharmacokinetics of antimony in the bone marrow of dogs with visceral leishmaniasis and on the ability of LMA to eliminate parasites from this tissue. Dogs naturally infected with Leishmania chagasi received 4 intravenous doses of either LMA (6.5 mg antimony/kg body weight, N = 9), or empty liposomes (at the same lipid dose as LMA, N = 9) at 4-day intervals. A third group of animals was untreated (N = 8). Before each administration and at different times after treatment, bone marrow was obtained and analyzed for antimony level (LMA group) by electrothermal atomic absorption spectrometry, and for the presence of... |
| Tipo: Info:eu-repo/semantics/other |
Palavras-chave: Liposome; Meglumine antimoniate; Pharmacokinetics; Leishmaniasis; Dogs; Bone marrow. |
| Ano: 2005 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2005001200017 |
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| Frézard,F.; Michalick,M.S.M.; Soares,C.F.; Demicheli,C.. |
| The antimonial drug, meglumine antimoniate, was successfully encapsulated in dehydration-rehydration vesicles and in freeze-dried empty liposomes (FDELs). High encapsulation efficiencies (from 28 to 58%) and low weight ratios of lipids to encapsulated antimony (from 1:0.15 to 1:0.3) were achieved. These formulations, contrary to those obtained by conventional methods, can be stored as intermediate lyophilized forms and reconstituted just before use. The efficacy of FDEL-encapsulated meglumine antimoniate was evaluated in hamsters experimentally infected with Leishmania chagasi. A significant reduction of liver parasite burdens was observed in animals treated with this preparation, when compared to control animals treated with empty liposomes. In contrast,... |
| Tipo: Info:eu-repo/semantics/other |
Palavras-chave: Liposomes; Glucantime; Meglumine antimoniate; Leishmaniasis; Encapsulation. |
| Ano: 2000 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X2000000700016 |
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