Sesquiterpene lactone in nanostructured parenteral dosage form is efficacious in experimental Chagas disease.

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dc.contributor.authorBranquinho, Renata Tupinambá
dc.contributor.authorMosqueira, Vanessa Carla Furtado
dc.contributor.authorSilva, Jaquelline Carla Valamiel de Oliveira e
dc.contributor.authorSilva, Marianne Rocha Simões
dc.contributor.authorGuimarães, Dênia Antunes Saúde
dc.contributor.authorLana, Marta de
dc.date.accessioned2017-03-10T11:52:45Z
dc.date.available2017-03-10T11:52:45Z
dc.date.issued2014
dc.description.abstractThe drugs available for Chagas disease treatment are toxic and ineffective. We studied the in vivo activity of a new drug, lychnopholide (LYC). LYC was loaded in nanocapsules (NC), and its effects were compared to free LYC and benznidazole against Trypanosoma cruzi. Infected mice were treated in the acute phase at 2.0 mg/kg/day with free LYC, LYC-poly- -caprolactone NC (LYC-PCL), and LYC-poly(lactic acid)-co-polyethylene glycol NC (LYC-PLA-PEG) or at 50 mg/kg/day with benznidazole solution by the intravenous route. Animals infected with the CL strain, treated 24 h after infection for 10 days, evaluated by hemoculture, PCR, and enzyme-linked immunosorbent assay exhibited a 50% parasitological cure when treated with LYC-PCL NC and 100% cure when treated with benznidazole, but 100% of the animals treated during the prepatent period for 20 days with these formulations or LYC-PLA-PEG NC were cured. In animals with the Y strain treated 24 h after infection for 10 days, only mice treated by LYC-PCL NC were cured, but animals treated in the prepatent period for 20 days exhibited 100, 75, and 62.5% cure when treated with LYC-PLA-PEG NC, benznidazole, and LYC-PCL NC, respectively. Free LYC reduced the parasitemia and improved mice survival, but no mice were cured. LYC-loaded NC showed higher cure rates, reduced parasitemia, and increased survival when used in doses 2five times lower than those used for benznidazole. This study confirms that LYC is a potential new treatment for Chagas disease. Furthermore, the long-circulating property of PLA-PEG NC and its ability to improve LYC efficacy showed that this formulation is more effective in reaching the parasite in vivo.pt_BR
dc.identifier.citationBRANQUINHO, R. T. et al. Sesquiterpene lactone in nanostructured parenteral dosage form is efficacious in experimental Chagas disease. Antimicrobial Agents And Chemotherapy, v. 58, p.2067-2075, 2014. Disponível em: <http://aac.asm.org/content/58/4/2067.long>. Acesso em: 10 jan. 2017.pt_BR
dc.identifier.doihttps://doi.org/10.1128/AAC.00617-13
dc.identifier.urihttp://www.repositorio.ufop.br/handle/123456789/7347
dc.identifier.uri2http://aac.asm.org/content/58/4/2067.longpt_BR
dc.language.isoen_USpt_BR
dc.rightsrestritopt_BR
dc.titleSesquiterpene lactone in nanostructured parenteral dosage form is efficacious in experimental Chagas disease.pt_BR
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