Dissolution enhancement of Enzalutamide by solid dispersion approach: Development, characterization and ex-vivo intestinal absorption study

Kunal Bagul; Atishkumar Mundada

doi:10.53730/ijhs.v6nS4.11802

Authors

Kunal Bagul
kuba05@yahoo.co.in
Research Scholar, SNJB’s Shriman Sureshdada Jain College of Pharmacy, Nemi Nagar, Chandwad, Dist. Nashik-423 101, Affiliated to Savitribai Phule Pune University, Pune, Maharashtra, India
Atishkumar Mundada Research Guide, SNJB’s Shriman Sureshdada Jain College of Pharmacy, Nemi Nagar, Chandwad, Dist. Nashik-423 101, Affiliated to Savitribai Phule Pune University, Pune, Maharashtra, India

Keywords:

solid dispersion, dissolution enhancement, solvent evaporation, BCS II, spray drying, ternary solid dispersion

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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