Efficient Enhancement in Itraconazole Solubility through its Cyclodextrin-Water Soluble Polymer Ternary Inclusion Complexes

The aim of this work is the enhancement of the hydrosolubility behaviour of a poorly soluble, weakly basic drug, using itraconazole (ITZ) as a case example. Binary inclusion complexes of ITZ with β-cyclodextrin (β-CD) are prepared in 1:2 molar ratios of ITZ to β-CD by co-evaporation method. Both solubility and dissolution behaviour are compared with that of the pure drug. Ternary complexes can be obtained by adding the polyvinylpirrolidone (PVP) which is a highly water soluble polymer, in the ITZ/ β-CD complex formation. Actually, Solid state analysis is performed for all formulations and for pure ITZ applying the Fourier transforms infrared (FT-IR) spectroscopy, powder X-ray diffraction (pX-RD) and differential scanning calorimetry (DSC). Solubility tests indicate that with all formulation, the solubility of ITZ formed with β-CD or β-CD and PVP proved to be increased. The obtained results show that the pure drug has a poor dissolution property, and the ternary inclusion complexes resulted in fast and extensive release of ITZ. Keywords: Itraconazole, β-cyclodextrin, polyvinylpyrrolidone.