RT Journal Article
T1 Inclusion complex of ITH12674 with2-hydroxypropyl-beta-cyclodextrin: Preparation, physical characterization and pharmacological effect
A1 Michalska Dziama, Patrycja
A1 Wojnicz, Aneta
A1 Ruiz-Nuño, Ana
A1 Abril, Sheila
A1 Buendia, Izaskun
A1 León Martínez, Rafael
AB 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.
SN 0144-8617
YR 2016
FD 2016-09-24
LK https://hdl.handle.net/20.500.14352/95750
UL https://hdl.handle.net/20.500.14352/95750
LA eng
NO 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.
NO European Commission-ERC
NO Instituto de Salud Carlos III
NO Fundación FIPSE
NO Instituto-Fundación Teófilo Hernando
DS Docta Complutense
RD 21 jul 2024