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

Yiqiong Pu¹, Xitong Zhang², Qi Zhang³

¹Experiment Center for Teaching and Learning, Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Pudong New District, Shanghai 201203, China. puyiq@163.com.

Molecules (Basel, Switzerland)

|October 25, 2016

Summary

We developed an efficient phospholipid complex (PPD-PLC) to improve the solubility and stability of 20(S)-Protopanaxadiol (PPD). This formulation strategy enhances PPD

Keywords:

20(S)-protopanaxadiol DSC central composite design molecular docking phospholipid complex

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Area of Science:

Pharmacology and Drug Delivery
Natural Product Chemistry
Materials Science

Background:

20(S)-Protopanaxadiol (PPD), a ginseng-derived compound, exhibits diverse therapeutic effects including cardioprotective, neuroprotective, and anticancer activities.
The clinical utility of PPD is significantly hindered by its poor aqueous solubility, a common challenge for many bioactive natural products.

Purpose of the Study:

To optimize and develop an efficient phospholipid complex (PPD-PLC) of 20(S)-Protopanaxadiol (PPD) to overcome its solubility limitations.
To prepare and evaluate PPD-PLC-loaded dry suspension (PPD-PLC-SU) for improved in vitro performance and stability.

Main Methods:

Utilized central composite design and response surface analysis for optimizing PPD-PLC preparation.
Characterized PPD-PLC using techniques like DSC, XRD, FTIR, NMR, and molecular docking.
Assessed in vitro dissolution behavior and stability of PPD-PLC and PPD-PLC-SU.

Main Results:

Optimized PPD-PLC demonstrated a 6.53-fold increase in aqueous solubility and a 1.53-fold increase in n-octanol solubility.
In vitro evaluations showed significantly improved dissolution extents and rates for both PPD-PLC and PPD-PLC-SU.
PPD-PLC-SU exhibited enhanced stability compared to free PPD under various conditions.

Conclusions:

Phospholipid complex technology is a viable strategy for enhancing the hydrophilicity and lipophilicity of BCS Class II drugs like PPD.
The developed PPD-PLC and PPD-PLC-SU formulations offer a promising approach for improving the bioavailability and therapeutic efficacy of PPD.
This formulation strategy holds potential for overcoming solubility challenges in natural product drug development.