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Optimization and evaluation of resveratrol amorphous solid dispersions with a novel polymeric system
Gangqi Han1,2,3, Bing Wang3,4, Mengli Jia3
1State Key Laboratory of Bio-based Material and Green Papermaking (LBMP), Qilu University of Technology (Shandong Academy of Sciences), Jinan, Shandong, China.
Mathematical Biosciences and Engineering : MBE
|July 8, 2022
Summary
This study optimized resveratrol amorphous solid dispersions using a novel poly (vinyl pyrrolidone) and carboxymethyl chitosan blend. The new formulation significantly enhanced resveratrol
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Amorphous solid dispersions enhance solubility of poorly water-soluble drugs.
- Single polymers often provide limited solubility and stability enhancement.
- Novel binary polymeric blends offer potential for improved drug formulation.
Purpose of the Study:
- To optimize and evaluate resveratrol (Res) amorphous solid dispersions using a novel poly (vinyl pyrrolidone) (PVP) and carboxymethyl chitosan (CMCS) system.
- To investigate the influence of CMCS ratio, Res ratio, and surfactant concentration on Res release.
- To assess the physical stability and dissolution characteristics of the optimized dispersions.
Main Methods:
- Computer optimization and contour plots were used to determine optimal formulation parameters.
- Fourier transform infrared spectroscopy (FTIR) analyzed drug-polymer interactions.
- Scanning electron microscopy (SEM), X-ray diffraction (XRD), and modulated differential scanning calorimetry (MDSC) assessed physical properties and stability.
- Dissolution testing evaluated drug release and apparent solubility.
Main Results:
- Optimized formulation variables predicted using computer optimization: CMCS ratio (X1) = 0.17, Res ratio (X2) = 0.10, and Tween 80 concentration (X3) = 2.94.
- FTIR confirmed hydrogen bonding between Res and both PVP and CMCS.
- SEM, XRD, and MDSC confirmed the amorphous state of Res and demonstrated excellent physical stability without phase separation during storage.
- Dissolution testing revealed a greater than fourfold increase in apparent solubility, with sustained high solubility for 90 days.
Conclusions:
- The novel binary polymeric system of PVP and CMCS effectively enhances resveratrol's in vitro dissolution and solubility.
- The optimized ternary dispersions exhibit excellent physical stability, making them a promising formulation strategy for poorly water-soluble drugs.
- CMCS represents a novel and effective carrier in combination with PVP for improving drug solubility and stability.
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