Amorphous Pterostilbene Delivery Systems Preparation-Innovative Approach to Preparation Optimization.

Area of Science:

• Materials Science
• Pharmaceutical Technology
• Biochemistry

Background:

• Pterostilbene (PTR) is a natural compound with potent antioxidant properties but limited bioavailability.
• Improving the solubility and antioxidant efficacy of PTR is crucial for its therapeutic applications.

Purpose of the Study:

• To enhance the solubility and antioxidant activity of pterostilbene (PTR).
• To develop a novel amorphous solid dispersion (ASD) of PTR using Soluplus® (SOL) via a green, low-cost dry milling process.

Main Methods:

• Differential Scanning Calorimetry (DSC) and mathematical models were used for formulation optimization.
• Dry milling was employed for the green amorphization process.
• X-ray Powder Diffraction (XRPD), Scanning Electron Microscopy (SEM), and Fourier-Transform Infrared Spectroscopy (FT-IR) were used for characterization.

Main Results:

• Full amorphization of PTR in SOL was confirmed by XRPD at 1:2 and 1:5 weight ratios.
• SEM indicated smaller particle size and larger surface area for the ASD systems.
• Apparent solubility increased ~37-fold and ~28-fold for PTR-SOL 1:2 and 1:5 w/w, respectively.
• Antioxidant activity was significantly improved, with the 1:2 w/w system showing the best performance.

Conclusions:

• Dry milling is an effective green method for creating stable amorphous solid dispersions of PTR with SOL.
• The developed ASD significantly enhances PTR's apparent solubility and antioxidant activity.
• The PTR-SOL 1:2 w/w ASD formulation is a promising approach for improving pterostilbene's therapeutic potential.