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- Title
Designing and monitoring microstructural properties of oligosaccharide/co-solvent ternary complex particles to improve benznidazole dissolution.
- Authors
de Melo, Polyanne N.; de Caland, Lilia B.; Fernandes-Pedrosa, Matheus F.; da Silva-Júnior, Arnóbio Antônio
- 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.
- Subjects
CHAGAS' disease treatment; DRUG efficacy; DRUG solubility; SOLVENTS; DISSOLUTION (Chemistry); DISPERSION (Chemistry)
- Publication
Journal of Materials Science, 2018, Vol 53, Issue 4, p2472
- ISSN
0022-2461
- Publication type
Article
- DOI
10.1007/s10853-017-1720-3