Inclusion complex of ITH12674 with2-hydroxypropyl-beta-cyclodextrin: Preparation, physical characterization and pharmacological effect
dc.contributor.author | Michalska Dziama, Patrycja | |
dc.contributor.author | Wojnicz, Aneta | |
dc.contributor.author | Ruiz-Nuño, Ana | |
dc.contributor.author | Abril, Sheila | |
dc.contributor.author | Buendia, Izaskun | |
dc.contributor.author | León Martínez, Rafael | |
dc.date.accessioned | 2024-01-29T08:53:23Z | |
dc.date.available | 2024-01-29T08:53:23Z | |
dc.date.issued | 2016-09-24 | |
dc.description.abstract | ITH12674 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.department | Depto. de Química en Ciencias Farmacéuticas | |
dc.description.faculty | Fac. de Farmacia | |
dc.description.refereed | TRUE | |
dc.description.sponsorship | European Commission-ERC | |
dc.description.sponsorship | Instituto de Salud Carlos III | |
dc.description.sponsorship | Fundación FIPSE | |
dc.description.sponsorship | Instituto-Fundación Teófilo Hernando | |
dc.description.status | pub | |
dc.identifier.citation | Michalska 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.doi | 10.1016/j.carbpol.2016.09.072 | |
dc.identifier.issn | 0144-8617 | |
dc.identifier.officialurl | https://doi.org/10.1016/j.carbpol.2016.09.072 | |
dc.identifier.uri | https://hdl.handle.net/20.500.14352/95750 | |
dc.issue.number | 10 | |
dc.journal.title | Carbohydrate Polymers | |
dc.language.iso | eng | |
dc.page.final | 104 | |
dc.page.initial | 94 | |
dc.relation.projectID | info:eu-repo/grantAgreement/PCIG11-GA-2012-322156 | |
dc.relation.projectID | info: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.projectID | info:eu-repo/grantAgreement/MICINN//CP11%2F00165/ES/CP11%2F00165/ | |
dc.relation.projectID | info:eu-repo/grantAgreement/2015-03-1282 | |
dc.relation.projectID | info:eu-repo/grantAgreement/12-00001344-15 | |
dc.relation.projectID | info:eu-repo/grantAgreement/MECD//FPU13%2F03737/ES/FPU13%2F03737/ | |
dc.relation.projectID | info:eu-repo/grantAgreement/MECD//FPU12%2F02220/ES/FPU12%2F02220/ | |
dc.relation.projectID | info:eu-repo/grantAgreement/MECD//FPU14%2F05224/ES/FPU14%2F05224/ | |
dc.rights.accessRights | restricted access | |
dc.subject.cdu | 615:54 | |
dc.subject.cdu | 615.31 | |
dc.subject.keyword | ITH12674 | |
dc.subject.keyword | 2-Hydroxypropyl-β-cyclodextrin | |
dc.subject.keyword | Nrf2 inducer | |
dc.subject.keyword | Inclusion complex | |
dc.subject.ucm | Farmacología (Farmacia) | |
dc.subject.ucm | Química farmaceútica | |
dc.subject.unesco | 3209.99 Otras | |
dc.title | Inclusion complex of ITH12674 with2-hydroxypropyl-beta-cyclodextrin: Preparation, physical characterization and pharmacological effect | |
dc.type | journal article | |
dc.type.hasVersion | VoR | |
dc.volume.number | 157 | |
dspace.entity.type | Publication | |
relation.isAuthorOfPublication | 298927e3-bd5b-46ad-bdbe-b818ade8cfb1 | |
relation.isAuthorOfPublication | 7093c6ce-e368-44f0-a993-8f7212cb1c2a | |
relation.isAuthorOfPublication.latestForDiscovery | 298927e3-bd5b-46ad-bdbe-b818ade8cfb1 |
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