Maximiano, Flávia PiresPaula, Lívia Maria deFigueiredo, Vivian PaulinoAndrade, Isabel Mayer deSilva, André Talvani Pedrosa daBarreto, Lívia Cristina Lira de SáBahia, Maria TerezinhaCunha Filho, Marcílio Sérgio Soares da2015-01-282015-01-282011MAXIMIANO, 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: <http://www.sciencedirect.com/science/article/pii/S0939641111000877>. Acesso em: 08 nov. 2014.0939-6411http://www.repositorio.ufop.br/handle/123456789/4418Benznidazole (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.en-USBenznidazoleChagas diseaseSolvent change precipitationDissolution rateMicrocrystalsArtigo publicado em periodicoO periódico European Journal of Pharmaceutics and Biopharmaceutics concede permissão para depósito deste artigo no Repositório Institucional da UFOP. Número da licença: 3517690950523.https://doi.org/10.1016/j.ejpb.2011.03.003