Abstract

Inclusion complexes of dexamethasone acetate (DMA) with β-cyclodextrin ( β-CD), hydroxypropyl- β-cyclodextrin (HP- β-CD) and γ-cyclodextrin ( γ-CD) in water were characterised by the solubility method, spectroscopy ( 1H-NMR) and differential scanning calorimetry (DSC). In addition, the influence of complexation on DMA stability was assessed by a thermal stress method. Complexation with CDs increased the DMA aqueous solubility. The stoichiometric ratios of the inclusion complexes were 1:1, 1:2 and 1:1 for β-, γ- and HP- β-CD, respectively. Complexation with β-CD and HP- β-CD increased the DMA stability 5- and 12-fold, respectively. The 1H-NMR studies showed that the DMA `A' ring was included in the cavity of the CDs. The oil–water partition coefficient values of the DMA decreased significantly when complexes were formed, suggesting that the partition of this drug into lipophilic membranes may be improved. These observations suggest that DMA/CD complexes may be an attractive and practical procedure to modify drug physicochemical properties for use in delivery systems.

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