Caracterização de produtos de complexação furazolidona/β-ciclodextrina
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Data
2025-03-31
Autores
Robran, Lukas Eller
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Universidade Federal do Espírito Santo
Resumo
Cyclodextrins are cyclic oligosaccharides used in the formation of inclusion complexes. For these, hydrophobic molecules are included in the cavity of cyclodextrins, as a pharmacotechnical strategy to get around issues such as low water solubility, and low active pharmaceutical ingredient (API) stability. This characteristic is of extreme importance for the pharmaceutical industry, due to the improvement of drug bioavailability. Furazolidone is an antimicrobial and antiprotozoal API that has been withdrawn from use in humans in Brazil thanks to its toxicity. However, the API has been the subject of studies in the attempt to reposition its use in humans and animals, including as a leshmanicidal agent, contributing to fight this neglected disease endemic in low wage populations. Unfortunately, its insolubility in water causes low bioavailability. This problem motivates the study of its complexation with cyclodextrins, something not yet widely studied for this drug. Works of this kind are relevant due to being in line with Sustainable Development Goal 3 from the United Nations 2030 Agenda. In this study, different mixtures of β-cyclodextrin and furazolidone were prepared by kneading, dyalisis followed by freeze-drying, stove drying and physical mixture. The prepared mixtures were characterized by X-ray diffraction (XRD), thermal analysis and solid state nuclear magnetic resonance (NMR) to check for changes in physical, chemical or strucutral features caused by different preparation procedures. Some evidence for these modifications was observed, such as furazolidone melting peak reduction and variations of cristallinity of both compounds. The lattice parameters obtained with X-ray diffraction showed no significant changes for the different mixtures, and the diffraction peaks have noticeable changes in intensity. Differential thermal analysis showed the amount of crystalline furazolidone melting was reduced in kneaded and stove-dried mixtures. Solid-state 1H and 13C NMR analysis revealed reduction in 1H spin-lattice relaxation times (T1) and 1H spin-lattice relaxation times in the rotating frame (T1ρ). However those values were still significantly distinct for β-ciclodextrin and furazolidone, indicating possible immiscibility of the these components at the molecular level and that an inclusion complex was not formed.
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Fármacos , Ressonância magnética nuclear no estado sólido , Difração de raios X