Fabrication of baicalin solid dispersion using the supercritical anti-solvent technology: optimization,...

Area of Science:

• Pharmacology
• Materials Science
• Chemical Engineering

Background:

• Baicalin, a potent flavonoid glycoside from Scutellaria baicalensis, faces clinical limitations due to poor solubility and bioavailability.
• Enhancing baicalin's physicochemical properties is crucial for its therapeutic applications.

Purpose of the Study:

• To prepare amorphous solid dispersions of baicalin using a supercritical anti-solvent (SAS) process.
• To optimize the SAS process for enhanced baicalin dissolution and bioavailability.
• To evaluate the antimicrobial properties of the prepared baicalin solid dispersion.

Main Methods:

• Supercritical anti-solvent (SAS) process utilizing optimized parameters (temperature, pressure, CO2 flow rate) based on Box-Behnken Design (BBD).
• Characterization of the amorphous solid dispersion using Scanning Electron Microscopy (SEM), Fourier-Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and X-ray Diffraction (XRD).
• In vitro dissolution testing and in vivo pharmacokinetic studies in rats.

Main Results:

• The SAS process successfully produced amorphous baicalin solid dispersions (BASD).
• BASD exhibited a 9.4-fold increase in solubility at pH 6.8 and a 1.8-fold increase in bioavailability compared to raw baicalin.
• BASD demonstrated significant inhibitory effects against Bacillus subtilis and Escherichia coli.

Conclusions:

• The BBD-optimized SAS process is effective for preparing amorphous baicalin solid dispersions with improved solubility and bioavailability.
• The enhanced baicalin formulation shows potential for improved therapeutic efficacy and antimicrobial applications.