Corticosteroid microparticles produced by supercritical-assisted atomization: process optimization, product...

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Chemical Engineering

Background:

• Microparticle production is crucial for drug delivery systems.
• Supercritical-assisted atomization (SAA) offers a novel approach for particle engineering.
• Controlling particle size, morphology, and crystallinity impacts drug efficacy.

Purpose of the Study:

• To develop and optimize the production of dexamethasone and dexamethasone acetate microparticles using SAA.
• To investigate the influence of process parameters on particle characteristics.
• To evaluate the in vitro activity and drug degradation after SAA processing.

Main Methods:

• Solubilization of supercritical carbon dioxide in a drug-containing liquid solution.
• Atomization of the ternary mixture through a nozzle to form submicroparticles.
• Systematic variation of organic solvents (methanol, acetone), solute concentration, and CO2 flow rate ratio.
• Analysis of particle morphology, size distribution (PSD), crystallinity, and surface area.
• In vitro testing of drug activity on pro-inflammatory cytokine release.

Main Results:

• Spherical corticosteroid microparticles (0.5–1.2 µm) with narrow PSDs were produced.
• No drug degradation was observed; residual solvent levels were within acceptable limits (300-500 ppm).
• SAA-processed glucocorticoids retained their in vitro activity; dexamethasone showed improved performance.

Conclusions:

• SAA is an effective method for producing dexamethasone and dexamethasone acetate microparticles with controlled properties.
• The SAA process preserves drug integrity and can enhance therapeutic efficacy.
• Optimized SAA parameters yield high-quality microparticles suitable for pharmaceutical applications.