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Open AccessArticle

20(S)-Protopanaxadiol Phospholipid Complex: Process Optimization, Characterization, In Vitro Dissolution and Molecular Docking Studies

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Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China
2
School of Pharmacy, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China
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Zhejiang BioAsia Institute of Life Science, No. 1938 Xinqun Road, Economic and Technical Development Zone, Pinghu 314200, China
4
Division of Life Science and Center for Chinese Medicine, The Hong Kong University of Science and Technology, Clear Water Bay Road, Hong Kong, China
*
Authors to whom correspondence should be addressed.
Academic Editors: Thomas Efferth and Derek J. McPhee
Molecules 2016, 21(10), 1396; https://doi.org/10.3390/molecules21101396
Received: 17 July 2016 / Revised: 7 October 2016 / Accepted: 13 October 2016 / Published: 19 October 2016
(This article belongs to the Section Natural Products Chemistry)
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 and n-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. View Full-Text
Keywords: 20(S)-protopanaxadiol; phospholipid complex; central composite design; DSC; molecular docking 20(S)-protopanaxadiol; phospholipid complex; central composite design; DSC; molecular docking
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Pu, Y.; Zhang, X.; Zhang, Q.; Wang, B.; Chen, Y.; Zang, C.; Wang, Y.; Dong, T.T.-X.; Zhang, T. 20(S)-Protopanaxadiol Phospholipid Complex: Process Optimization, Characterization, In Vitro Dissolution and Molecular Docking Studies. Molecules 2016, 21, 1396.

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