20(S)-Protopanaxadiol phospholipid complex: Process optimization, characterization, in vitro dissolution and molecular docking studies

Abstract

20(S)-Protopanaxadiol (PPD), a bioactive compound extracted from ginseng, possesse cardioprotective, neuroprotective, anti-inflammatory, antiestrogenic, anticancer and anxiolytic effects However, the clinical application of PPD is limited by its weak aqueous solubility. In this study we optimized an efficient method of preparing its phospholipid complex (PPD-PLC) using central composite design and response surface analysis. The prepared PPD-PLC was characterize by differential scanning calorimetric, powder X-ray diffraction, Fourier-Transformed infrare spectroscopy and nuclear magnetic resonance analyses associated with molecular docking calculation The equilibrium solubility of PPD-PLC in water and n-octanol increased 6.53-and 1.53-Times respectively. Afterwards, using PPD-PLC as the intermediate, the PPD-PLC-loaded dry suspensio (PPD-PLC-SU) was prepared with our previous method. In vitro evaluations were conducted o PPD-PLC and PPD-PLC-SU, including dissolution behaviors and stability properties under differen conditions. Results of in vitro dissolution behavior revealed the improved dissolution extents an rates of PPD-PLC and PPD-PLC-SU (p < 0.05). Results of the formulation stability investigatio also exposed the better stability of PPD-PLC-SU compared with free PPD. Therefore, phospholipi complex technology is a useful formulation strategy for BCS II drugs, as it could effectively improv their hydrophilicity and lipophilicity.