Benznidazole microcrystal preparation by solvent change precipitation and in vivo evaluation in the treatment of Chagas disease.

• Autor(a) principal: Maximiano, Flávia Pires
• Data de Publicação: 2011
• Outros Autores: 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
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Institucional da UFOP
• Texto Completo: http://www.repositorio.ufop.br/handle/123456789/4418; https://doi.org/10.1016/j.ejpb.2011.03.003
• topic: Benznidazole; Chagas disease; Solvent change precipitation; Dissolution rate; Microcrystals

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.