Elucidating the complexation of nifurtimox with cyclodextrins

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dc.creatorBedogni, Giselle Rocio
dc.creatorArrua, Eva Carolina
dc.creatorSeremeta, Katia Pamela
dc.creatorOkulik, Nora Beatriz
dc.creatorSalomon, Claudio Javier
dc.date2023-07
dc.descriptionChagas disease or American Trypanosomiasis, caused by the parasite Trypanosoma cruzi, is an endemic neglected infection found in 21 countries across Latin America. To date, nifurtimox is one of the only two drugs approved to treat Chagas disease but exhibits serious concerns related to its low aqueous solubility and erratic bioavailability. Thus, the aim of this work was to evaluate whether the formation of complexes with βcyclodextrin and sulfobutylether-β-cyclodextrin would improve drug solubility and dissolution rate. Drug-cyclodextrin interactions in solid-state were analyzed by differential scanning calorimetry, X-ray diffractometry, infrared spectroscopy, and nuclear magnetic resonance. The systems were characterized in solution by means of phase solubility, dissolution, and kinetic studies. Phase solubility study showed an AL-type diagram indicating the formation of inclusion complex in a 1:1 M ratio. The drug dissolution rate from sulfobutylether-β-cyclodextrin complexes was faster than that of the β-cyclodextrin complexes. The modification of the endothermic peak of nifurtimox revealed the presence of interactions between the drug and CDs. The crystalline character of the drug was greatly diminished after complexation with sulfobutylether-β-cyclodextrin. Microscopy evaluation revealed the formation of new structures of the solid particles, which suggest strong interactions between the drug and the carriers. The 1H and 13C nuclear magnetic resonance confirmed that the drug was included in the carriers. The selected nifurtimox complex stored at 25 °C and 40 °C during 6 months showed a remarkable stability in terms of drug dissolution and crystallinity.
dc.descriptionFil: Bedogni, Giselle Rocio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina
dc.descriptionFil: Arrua, Eva Carolina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro de Investigación y Desarrollo en Materiales Avanzados y Almacenamiento de Energía de Jujuy - Universidad Nacional de Jujuy. Centro de Investigación y Desarrollo en Materiales Avanzados y Almacenamiento de Energía de Jujuy - Gobierno de la Provincia de Jujuy. Centro de Investigación y Desarrollo en Materiales Avanzados y Almacenamiento de Energía de Jujuy; Argentina
dc.descriptionFil: Seremeta, Katia Pamela. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Chaco Austral. Departamento de Ciencias Básicas y Aplicadas; Argentina
dc.descriptionFil: Okulik, Nora Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Chaco Austral. Departamento de Ciencias Básicas y Aplicadas; Argentina
dc.descriptionFil: Salomon, Claudio Javier. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Departamento de Farmacia; Argentina
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dc.identifierhttp://hdl.handle.net/11336/224030
dc.identifierBedogni, Giselle Rocio; Arrua, Eva Carolina; Seremeta, Katia Pamela; Okulik, Nora Beatriz; Salomon, Claudio Javier; Elucidating the complexation of nifurtimox with cyclodextrins; Elsevier Science; Journal of Molecular Liquids; 382; 1218; 7-2023; 1-12
dc.identifier0167-7322
dc.identifierCONICET Digital
dc.identifierCONICET
dc.languageeng
dc.publisherElsevier Science
dc.relationinfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0167732223006554
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.molliq.2023.121852
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.rightshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.subjectNIFURTIMOX
dc.subjectCYCLODEXTRINS
dc.subjectFAST DISSOLUTION
dc.subjectSOLID-STATE
dc.subjecthttps://purl.org/becyt/ford/1.4
dc.subjecthttps://purl.org/becyt/ford/1
dc.titleElucidating the complexation of nifurtimox with cyclodextrins
dc.typeinfo:eu-repo/semantics/article
dc.typeinfo:ar-repo/semantics/artículo
dc.typeinfo:eu-repo/semantics/publishedVersion
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