Inclusion complex of ITH12674 with2-hydroxypropyl-beta-cyclodextrin: Preparation, physical characterization and pharmacological effect

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dc.contributor.authorMichalska Dziama, Patrycja
dc.contributor.authorWojnicz, Aneta
dc.contributor.authorRuiz-Nuño, Ana
dc.contributor.authorAbril, Sheila
dc.contributor.authorBuendia, Izaskun
dc.contributor.authorLeón Martínez, Rafael
dc.date.accessioned2024-01-29T08:53:23Z
dc.date.available2024-01-29T08:53:23Z
dc.date.issued2016-09-24
dc.description.abstractITH12674 is a multitarget drug, designed to exert a dual “drug-prodrug” mechanism of action, able toinduce the phase II antioxidant and anti-inflammatory response for the treatment of brain ischemia.However, its physicochemical properties limit its potential preclinical development due to its low watersolubility and instability towards heat and pH variations. In order to improve its properties, we preparedthe inclusion complex of ITH12674 with 2-hydroxypropyl- -cyclodextrin (HP- -CD) by the freeze-drying method. The formation of the inclusion complex was confirmed by FT-IR spectroscopy, PXRD,DSC,1H NMR and SEM techniques. Experimental results showed that the inclusion complex enhanced itswater solubility and stability against heat, acidic and basic conditions. Furthermore, the inclusion com-plex, prepared in water solution, exerted the same potency to induce the phase II antioxidant response asthe pure ITH12674. Thus the formation of the inclusion complex with HP- -CD is a very effective methodto stabilize and solubilize the active compound for its future preclinical development.
dc.description.departmentDepto. de Química en Ciencias Farmacéuticas
dc.description.facultyFac. de Farmacia
dc.description.refereedTRUE
dc.description.sponsorshipEuropean Commission-ERC
dc.description.sponsorshipInstituto de Salud Carlos III
dc.description.sponsorshipFundación FIPSE
dc.description.sponsorshipInstituto-Fundación Teófilo Hernando
dc.description.statuspub
dc.identifier.citationMichalska P, Wojnicz A, Ruiz-Nuño A, Abril S, Buendia I, León R. Inclusion complex of ITH12674 with 2-hydroxypropyl-β-cyclodextrin: Preparation, physical characterization and pharmacological effect. Carbohydrate Polymers 2017;157:94–104. https://doi.org/10.1016/j.carbpol.2016.09.072.
dc.identifier.doi10.1016/j.carbpol.2016.09.072
dc.identifier.issn0144-8617
dc.identifier.officialurlhttps://doi.org/10.1016/j.carbpol.2016.09.072
dc.identifier.urihttps://hdl.handle.net/20.500.14352/95750
dc.issue.number10
dc.journal.titleCarbohydrate Polymers
dc.language.isoeng
dc.page.final104
dc.page.initial94
dc.relation.projectIDinfo:eu-repo/grantAgreement/PCIG11-GA-2012-322156
dc.relation.projectIDinfo:eu-repo/grantAgreement/MINECO//PI14%2F00372/ES/Compuestos muldidiana quirales para el tratamiento de enfermedades neurodegenerativas: ligandos de receptores nicotínicos, inductores de Nrf2 y anti-inflamatorios/
dc.relation.projectIDinfo:eu-repo/grantAgreement/MICINN//CP11%2F00165/ES/CP11%2F00165/
dc.relation.projectIDinfo:eu-repo/grantAgreement/2015-03-1282
dc.relation.projectIDinfo:eu-repo/grantAgreement/12-00001344-15
dc.relation.projectIDinfo:eu-repo/grantAgreement/MECD//FPU13%2F03737/ES/FPU13%2F03737/
dc.relation.projectIDinfo:eu-repo/grantAgreement/MECD//FPU12%2F02220/ES/FPU12%2F02220/
dc.relation.projectIDinfo:eu-repo/grantAgreement/MECD//FPU14%2F05224/ES/FPU14%2F05224/
dc.rights.accessRightsrestricted access
dc.subject.cdu615:54
dc.subject.cdu615.31
dc.subject.keywordITH12674
dc.subject.keyword2-Hydroxypropyl-β-cyclodextrin
dc.subject.keywordNrf2 inducer
dc.subject.keywordInclusion complex
dc.subject.ucmFarmacología (Farmacia)
dc.subject.ucmQuímica farmaceútica
dc.subject.unesco3209.99 Otras
dc.titleInclusion complex of ITH12674 with2-hydroxypropyl-beta-cyclodextrin: Preparation, physical characterization and pharmacological effect
dc.typejournal article
dc.type.hasVersionVoR
dc.volume.number157
dspace.entity.typePublication
relation.isAuthorOfPublication298927e3-bd5b-46ad-bdbe-b818ade8cfb1
relation.isAuthorOfPublication7093c6ce-e368-44f0-a993-8f7212cb1c2a
relation.isAuthorOfPublication.latestForDiscovery298927e3-bd5b-46ad-bdbe-b818ade8cfb1
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