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

Designing and monitoring microstructural properties of oligosaccharide/co-solvent ternary complex... 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. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Journal of Materials Science Springer Journals

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

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Publisher
Springer US
Copyright
Copyright © 2017 by Springer Science+Business Media, LLC
Subject
Materials Science; Materials Science, general; Characterization and Evaluation of Materials; Polymer Sciences; Continuum Mechanics and Mechanics of Materials; Crystallography and Scattering Methods; Classical Mechanics
ISSN
0022-2461
eISSN
1573-4803
D.O.I.
10.1007/s10853-017-1720-3
Publisher site
See Article on Publisher Site

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.

Journal

Journal of Materials ScienceSpringer Journals

Published: Oct 31, 2017

References

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