title: 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, possesses 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 a central composite design and response surface analysis. The prepared PPD-PLC was characterized by differential scanning calorimetric, powder X-ray diffraction, Fourier-transformed infrared spectroscopy and nuclear magnetic resonance analyses associated with molecular docking calculation. The equilibrium solubility of PPD-PLC in water andn-octanol increased 6.53- and 1.53-times, respectively. Afterwards, using PPD-PLC as the intermediate, the PPD-PLC-loaded dry suspension (PPD-PLC-SU) was prepared with our previous method. In vitro evaluations were conducted on PPD-PLC and PPD-PLC-SU, including dissolution behaviors and stability properties under different conditions. Results of in vitro dissolution behavior revealed the improved dissolution extents and rates of PPD-PLC and PPD-PLC-SU (p< 0.05). Results of the formulation stability investigation also exposed the better stability of PPD-PLC-SU compared with free PPD. Therefore, phospholipid complex technology is a useful formulation strategy for BCS II drugs, as it could effectively improve their hydrophilicity and lipophilicity.
authors: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. puyiq@163.com.
authors: Yiqiong
authors: Y
authors: Pu
authors: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. zhangxitong1990@126.com.
authors: Xitong
authors: X
authors: Zhang
authors: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. zhang645654@163.com.
authors: Qi
authors: Q
authors: Zhang
authors: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. annabel_cn@163.com.|School of Pharmacy, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. annabel_cn@163.com.
authors: Bing
authors: B
authors: Wang
authors: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. yuxi59shutcm@163.com.
authors: Yuxi
authors: Y
authors: Chen
authors: School of Pharmacy, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. zangchuanqi1991@sina.com.
authors: Chuanqi
authors: C
authors: Zang
authors: Zhejiang BioAsia Institute of Life Science, No. 1938 Xinqun Road, Economic and Technical Development Zone, Pinghu 314200, China. wyq@bioasia.com.cn.
authors: Yuqin
authors: Y
authors: Wang
authors: Division of Life Science and Center for Chinese Medicine, The Hong Kong University of Science and Technology, Clear Water Bay Road, Hong Kong, China. botina@ust.hk.
authors: Tina Ting-Xia
authors: TT
authors: Dong
authors: Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. zhangtdmj@hotmail.com.|School of Pharmacy, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. zhangtdmj@hotmail.com.
authors: Tong
authors: T
authors: Zhang
mesh_terms: D019540:Area Under Curve; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D008855:Microscopy, Electron, Scanning; D062105:Molecular Docking Simulation / Q000379:methods*; D015394:Molecular Structure; D010743:Phospholipids / Q000737:chemistry*; D033362:Powder Diffraction; D012502:Sapogenins / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction
chemical_list: D010743:Phospholipids; D012502:Sapogenins; C062916:protopanaxadiol
keywords: 20(S)-protopanaxadiol; DSC; central composite design; molecular docking; phospholipid complex