Next Article in Journal
Curcumin Shows Antiviral Properties against Norovirus
Previous Article in Journal
The Potential of Secondary Metabolites from Plants as Drugs or Leads against Protozoan Neglected Diseases—Part III: In-Silico Molecular Docking Investigations
Article Menu
Issue 10 (October) cover image

Export Article

Open AccessArticle
Molecules 2016, 21(10), 1396; doi:10.3390/molecules21101396

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

1
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
3
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
Received: 17 July 2016 / Revised: 7 October 2016 / Accepted: 13 October 2016 / Published: 19 October 2016
(This article belongs to the Section Natural Products)
View Full-Text   |   Download PDF [3887 KB, uploaded 19 October 2016]   |  

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 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
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

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.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top