Physicochemical and thermodynamic characterization of hydroxy pentacyclic triterpenoic acid/γ-cyclodextrin inclusion complexes

Abstract : Hydroxy pentacyclic triterpenoic acids (HPTAs) have been described to exhibit numerous pharmacological properties. They also exhibit poor hydrosolubility, thus affecting their potential clinical interest. The association of these active substances with cyclodextrins could be employed to improve some properties such as bioavailability and activity. 1:1 Inclusion complexes of ursolic, oleanolic and betulinic acids with γ-cyclodextrin were evaluated by DSC and 1H NMR spectroscopy. The apparent formation constants (Kf) of the formed complexes were determined using RP-HPLC. Thermodynamic parameters ΔGº, ΔHº and ΔSº were calculated with temperatures ranging from 25 to 45 °C to evaluate the complexation process. Finally the influence of γ-CD on the HPTA water solubility was investigated by phase-solubility studies.
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Journal of Inclusion Phenomena and Macrocyclic Chemistry, Springer Verlag, 2012, 73 (1-4), pp.341 - 347. 〈10.1007/s10847-011-0063-y〉
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https://hal.univ-lorraine.fr/hal-01650404
Contributeur : Raphaël Duval <>
Soumis le : mardi 28 novembre 2017 - 13:45:18
Dernière modification le : mardi 16 janvier 2018 - 10:24:44

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Stéphane Fontanay, Francine Kedzierewicz, Raphaël E. Duval, Igor Clarot. Physicochemical and thermodynamic characterization of hydroxy pentacyclic triterpenoic acid/γ-cyclodextrin inclusion complexes. Journal of Inclusion Phenomena and Macrocyclic Chemistry, Springer Verlag, 2012, 73 (1-4), pp.341 - 347. 〈10.1007/s10847-011-0063-y〉. 〈hal-01650404〉

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