The purpose of this study was to investigate the feasibility of a supercritical fluid process, called aerosol solvent extraction system (ASES), for producing solid-state inclusion complexes of itraconazole (ITR) with 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD). ITR was complexed with HP-beta-CD at temperatures of 35-55 degrees C, pressures of 83-140 bar, CO2 densities of 0.498-0.801 g/cm(3), and solution concentrations of 1-5% (w/v). The ASES-processed inclusion complex powders were observed to consist of agglomerates of very fine (100-500 nm) particles. From the experimental results of X-ray diffraction and differential scanning calorimetry, it was found that ITR intermolecularly interacted with the HP-beta-CD cavity, resulting in the formation of inclusion complex. Furthermore, the ASES-processed ITR/HP-beta-CD powders showed a significant enhancement in the ITR solubility (up to 753.6 mu g/mL) in an aqueous medium of pH 1.2. The aqueous solubility of ITR increased with pressure at a constant temperature, and we could obtain a relatively high solubility of 341 mu g/mL at 140 bar and 35 degrees C. In a solution concentration range of 1-5% (w/v), the solubility increased with decreasing concentration, yielding 289-407 mu g/mL. When the molar ratio of ITR to HP-beta-CD was varied from 1: 1 to 1:3, the ITR solubility increased with HP-beta-CD content, giving a value of 753.6 mu g/mL for the 1:3 ratio. For the ASES-processed ITRIHP-beta-CD powders, the percent dissolution of ITR also increased considerably and about 90% of ITR was dissolved within 5-10 min. (C) 2007 Elsevier B.V. All rights reserved.