A Study to Improve the Solubility and Dissolution of Itraconazole Using Peg Solid Dispersions

Abstract

Itraconazole is a broad-spectrum triazole antifungal drug extensively used in the treatment of systemic and superficial fungal infections. However, its therapeutic effectiveness is limited by its poor aqueous solubility and slow dissolution rate, which result in low and variable oral bioavailability. The present study was undertaken to improve the solubility and dissolution characteristics of itraconazole by formulating solid dispersions using polyethylene glycol (PEG) as a hydrophilic carrier. Solid dispersion technology is a widely accepted approach for enhancing the dissolution of poorly water-soluble drugs by increasing wettability, reducing particle size, and converting the drug into an amorphous or less crystalline state. Itraconazole solid dispersions were prepared using suitable drug-to-polymer ratios by the fusion method. The prepared formulations were evaluated for percentage yield, drug content, saturation solubility, and in vitro dissolution studies. Drug–polymer compatibility was assessed using Fourier Transform Infrared Spectroscopy (FTIR), while Differential Scanning Calorimetry (DSC) and Powder X-ray Diffraction (PXRD) were used to characterize the physical state of the drug. The dissolution profiles of the solid dispersions were compared with those of the pure drug and physical mixtures to determine the extent of enhancement.The results indicated that PEG-based solid dispersions significantly improved the solubility and dissolution rate of itraconazole compared with the pure drug. The enhanced performance was attributed to improved wettability, reduced crystallinity, and uniform dispersion of the drug within the hydrophilic polymer matrix. The optimized formulation exhibited the highest drug release and dissolution efficiency, suggesting its potential to improve oral bioavailability and therapeutic efficacy.