Dissolution Enhancement Of Itraconazole By Loading On Parteck SLC Mesoporous Silica Followed By Hot Melt Extrusion.

Abstract

The enhancement of oral bioavailability of poorly water-soluble drugs remains one of the most challenging aspects of drug development. Therefore formulation approaches are being explored to enhance bioavailability of poorly water-soluble drugs. Thus, this study suggests that a combined approach of loading mesoporous silica (Parteck® SLC 500) entrapment followed by solid dispersion with Poloxamer 188 by hot melt extrusion process successfully improved dissolution of Itraconazole.

 Among the various approaches, ITZ was loaded onto mesoporous silica (Parteck® SLC 500) via the incipient wetness impregnation method. The optimized drug-loaded batch was extruded with polyvinyl alcohol (PVA) and Poloxamer 188 in varying ratios. The formulations were characterized by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD). In-vitro dissolution studies were conducted to assess the drug release profiles.

The optimized formulation containing PVA and Poloxamer 188 in a 1:2 ratio demonstrated a 4.5-fold improvement in dissolution rate compared to pure ITZ, achieving 87% drug release within 20 minutes. DSC and XRD results confirmed the conversion of ITZ from a crystalline to an amorphous state. While FTIR results confirmed the absence of chemical interactions between ITZ and the excipients.

From the above results, it was concluded that the combination of mesoporous silica loading and HME proved to be an efficient method for enhancing ITZ dissolution, offering a robust approach for improving the bioavailability of poorly water-soluble drugs.