Enhancement of piperine solubility by solid dispersion using Kollidone VA64 and Soluplus as polymers: physicochemical characterization, molecular docking and cell viability assay.

Abstract

Piperine (PRN) is a water-insoluble alkaloidal drug reported for different biological activities. As part of this study, Kollidone VA64 (KLD) and Soluplus (SLP) were used as carriers to develop piperine solid dispersions (PRN SDs) to enhance their solubility. The stability constant of the drug-polymer composition was determined by the phase solubility study. PRN SDs were evaluated for dissolution and saturation solubility studies to select the optimized composition. SDs were evaluated for drug-polymer compatibility by Infra-red and nuclear magnetic spectroscopy. The drug crystallinity was evaluated by scanning electron microscopy and X-Ray diffraction method. Finally, a comparative cell viability assay was performed on the breast cancer cell line. The ternary system (PRN-KLD-SLP) depicted a significantly (p < 0.05) higher stability constant value than the binary system [PRN-KLD; (2.1 folds) and PRN-SLP (2.5-folds)]. An enhanced drug release (about 1.4-folds) was found from the ternary PRN SDs (F7-F9) than binary PRN SDs (F1-F6) and free PRN. The spectral analysis and molecular docking results confirm the formation of stable SDs. SEM and XRD results revealed conversion of crystalline PRN into an amorphous form. Cell viability data demonstrated a higher viability assay than the free PRN. Based on the study, we can say that the formation of ternary solid dispersion makes PRN more soluble and shows a better dissolution rate than the binary SDs.