Abstract

Enzalutamide (ENZ) is a BCS class II, fast crystallizing, a hydrophobic compound that has solubility limited absorption in vivo. Ternary solid dispersion of Enzalutamide was prepared with water-soluble polymers Soluplus (SOL) and Poloxamer P 188 (POL) by solvent evaporation spray drying technique. Initially, different ratios of Soluplus: Poloxamer and solvents were used to prepare Ternary solid dispersions of Enzalutamide and evaluated for the dissolution enhancement property. The prepared solid dispersion was characterized by FTIR spectroscopy, Differential scanning calorimetry (DSC), X-ray diffraction (XRD) analysis, Scanning electron microscopy (SEM), Particle size distribution (PSD) by Malvern and Physico-chemical analysis. FTIR spectroscopy shows that there was no interaction between the ENZ and polymers. DSC and XRD analysis show that conversion to amorphous form of ENZ in ternary SD, which enhances the dissolution rate. In vitro dissolution studies and Ex-vivo intestinal absorption studies clearly show that the prepared solid dispersion enhanced the dissolution and ex-vivo intestinal absorption of ENZ compared with pure ENZ.

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