Formulation and development of embelin liquisolid systems using quality by design approach

Abstract

The purpose of the present investigation was to improve dissolution properties of poorly water soluble herbal active ingredient, Embelin (EMB) by formulating liquisolid systems. The new mathematical model was employed for the preparation of the liquisolid systems. Drug loaded liquisolid systems were optimized by utilizing design of experiments (DoE) and principal component analysis (PCA) with carrier-coating ratio (X1) and drug concentration in liquid (X2) as factors. Angle of repose and percentage drug release in 30 min were selected as dependent variables. The liquisolid systems were prepared using Solutol® HS-15 in combination of Synperonic® PE/L61 in ratio of 1:1 as non-volatile liquid, Neusilin US2 as carrier and Aerosil 200 as coating material. The relationship between dependent and independent variables were further explicated through regression analysis and response surface plots. Prepared systems were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffraction studies. In-vitro dissolution results revealed significant enhancement in drug release properties from the formulations. Physicochemical characterization of liquisolid systems proposed reduction in drug crystallinity which might be ascribed for improvement in dissolution properties. Study demonstrated successful utilization of Solutol® HS-15 in combination of Synperonic® PE/L61 for dissolution enhancement of EMB.