Physical characterization and dissolution performance assessment of Etravirine solid dispersions prepared by spray drying process

ABSTRACT

The aim of the current exertion was to prepare Solid Dispersion of Etravirine by Spray drying technique to enhance aqueous solubility and dissolution rate. Solid dispersions [SD] of Etravirine were prepared using Copovidone and Povidone-Copovidone in dichloromethane and physical properties were characterized by Scanning electron microscopy [SEM], X-Ray diffractometry [PXRD], Fourier Transform Infrared Spectroscopy [FTIR], Differential Scanning Calorimetry [DSC]. SD's were evaluated for equilibrium solubility and in vitro drug release profile by dissolution testing. The diffraction and thermal patterns of solid dispersions indicated the conversion of crystalline Etravirine to amorphous form. The solubility of drug in SD's was appreciably more when evaluated against physical mixtures and intact Etravirine. Drug release characteristics were evaluated in three different media at different pH and found that drug release kinetic was best described by weibull mathematical model. Mean dissolution time [MDT] and Dissolution efficiency [DE %] in different media were evaluated for SDs. Statistical evaluation of dissolution data using Analysis Of Variance [ANOVA] single factor and t-Test Paired Two Sample for Means was applied for better understanding and evaluation