CHARACTERISATION OF INCLUSION COMPLEXES BETWEEN BIFONAZOLE AND DIFFERENT CYCLODEXTRINS IN SOLID AND SOLUTION STATE

Abstract

The aim of this study is to confirm the formation of inclusion complexes between bifonazole (BFZ) and different cyclodextrin (CD) derivatives. Bifonazole, an imidazole antifungal derivative,is a very hydrophobic compound, which is a major drawback in obtaining topical pharmaceutical formulations with optimal bioavailability. Cyclodextrins may increase local drug delivery by enhancing the drug release and/or permeation. The binary systems between bifonazole and cyclodextrins were prepared in two molar ratios by physical-mixture methods.The physicochemical properties of these complexes were studied by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) and nuclear magnetic resonance spectroscopy (NMR) methods. Results showed favourable molecular interaction between the components, in solid state and in solution. 1H NMR -CD titrations and molecular modelling study showed that the most stable complex was obtained when using γ-CD. The Job’s method and 2D NMR spectroscopy sustain the 2:1 stoichiometry of the BFZ:γ-CD complex.

Keywords

• bifonazole
• cyclodextrins
• differential scanning calorimetry
• fourier transform infrared spectroscopy
• 1h nmr -cd titrations