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Title: Benznidazole microcrystal preparation by solvent change precipitation and in vivo evaluation in the treatment of Chagas disease.
Authors: Maximiano, Flávia Pires
Paula, Lívia Maria de
Figueiredo, Vivian Paulino
Andrade, Isabel Mayer de
Silva, André Talvani Pedrosa da
Barreto, Lívia Cristina Lira de Sá
Bahia, Maria Terezinha
Cunha Filho, Marcílio Sérgio Soares da
Keywords: Benznidazole
Chagas disease
Solvent change precipitation
Dissolution rate
Issue Date: 2011
Citation: MAXIMIANO, F. P. et al. Benznidazole microcrystal preparation by solvent change precipitation and in vivo evaluation in the treatment of Chagas disease. European Journal of Pharmaceutics and Biopharmaceutics, v. 78, p. 377-384, 2011. Disponível em: <>. Acesso em: 08 nov. 2014.
Abstract: Benznidazole (BNZ) is traditionally used to treat Chagas disease. Despite its common use, BNZ has a poor water solubility and a variable bioavailability. The purpose of this study was to prepare BNZ microcrystals by solvent change precipitation and to study the effects of BNZ micronisation on therapeutic efficiency using a murine model of Chagas disease. The solvent change precipitation procedure was optimised in order to obtain stable and homogeneous particles with a small particle size, high yield and fast dissolution rate. The thermal and crystallographic analysis showed no polymorphic change in the microcrystals, and microscopy confirmed a significant reduction in particle size. A marked improvement in the drug dissolution rate was observed for micronised BNZ particles and BNZ tablets in comparison with untreated BNZ and commercial Rochagan_. In vivo studies showed a significant increase in the therapeutic efficacy of the BNZ microparticles, corroborating the dissolution results.
ISSN: 0939-6411
metadata.dc.rights.license: O periódico European Journal of Pharmaceutics and Biopharmaceutics concede permissão para depósito deste artigo no Repositório Institucional da UFOP. Número da licença: 3517690950523.
Appears in Collections:DECBI - Artigos publicados em periódicos

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