Characterization of Sulindac Solid Dispersion with Hydroxypropyl Cellulose Prepared by Hot Melt Extrusion

Abstract

The purpose of this study is to evaluate the applicability of solid dispersions prepared with hydroxypropyl cellulose (HPC). Solid dispersions were prepared with sulindac, a poorly water-soluble drug, and HPC of three different molecular weights using a hot melt extrusion method. Physicochemical properties of the solid dispersions were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and solubility studies. Permeability of sulindac was evaluated using the Caco-2 cell monolayer model. The results obtained by PXRD, DSC, and solubility studies showed that sulindac in the extrudate of sulindac/HPC (20/80 w/w) was completely amorphized and demonstrated better solubility than the drug alone. Permeability of sulindac across Caco-2 cell monolayers remarkably increased when the drug was solid-dispersed with the lowest molecular weight form of HPC (HPC-SSL). It has been concluded that HPC-SSL can be the most effective excipient in order to improve solubility and membrane permeability.