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Journal of Materials Science

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31-10-2017 | Chemical routes to materials

Designing and monitoring microstructural properties of oligosaccharide/co-solvent ternary complex particles to improve benznidazole dissolution

Authors: Polyanne N. de Melo, Lilia B. de Caland, Matheus F. Fernandes-Pedrosa, Arnóbio Antônio da Silva-Júnior

Published in: Journal of Materials Science | Issue 4/2018

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Abstract

Benznidazole (BNZ) is the main drug used for the treatment of Chagas disease. However, its low aqueous solubility limits its efficacy. In this study, we have prepared host–guest inclusion complexes of BNZ with beta-cyclodextrin (β-CD) in solid phase and assessed the influence of the co-solvents triethanolamine (TEA) and 1-methyl-2-pyrrolidone (NMP) for improving the drug dissolution performance. The physicochemical properties of prepared spray-dried (SD) particles and physical mixtures (PM) were carefully monitored using FTIR, XRD and SEM images. The used co-solvents affected β-CD–drug interactions, the structural properties and drug dissolution behavior of particles. TEA did not improve the solubilizing effect of β-CD, while NMP was able to enhance drug dissolution performance in both SD and PM complexes. These promising results support the use of specific co-solvents with CD as a new raw material for insoluble compounds. The studied solid dispersions showed promising features to improve BNZ efficacy against Chagas disease.

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Title: Designing and monitoring microstructural properties of oligosaccharide/co-solvent ternary complex particles to improve benznidazole dissolution
Authors: Polyanne N. de Melo
Lilia B. de Caland
Matheus F. Fernandes-Pedrosa
Arnóbio Antônio da Silva-Júnior
Publication date: 31-10-2017
Publisher: Springer US
Published in: Journal of Materials Science / Issue 4/2018
Print ISSN: 0022-2461
Electronic ISSN: 1573-4803
DOI: https://doi.org/10.1007/s10853-017-1720-3

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