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Overcoming Solubility Challenges: Micronization of Berberine Using the GAS Antisolvent Technique

Summary

Berberine is a traditional medicinal compound that could treat many diseases but doesn’t work well in the body because it doesn’t dissolve in water. Researchers used a special technique with pressurized carbon dioxide to break berberine into much smaller particles. This made the particles dissolve 18% better in water, which could make berberine-based medicines more effective at treating diabetes, high cholesterol, and other conditions.

Background

Berberine is a natural alkaloid used in traditional Chinese medicine with therapeutic potential for treating diabetes, cholesterol, and mental illnesses. However, its low water solubility limits bioavailability and absorption. Micronization techniques can increase surface area and dissolution rates to overcome these limitations.

Objective

This study aimed to investigate the use of supercritical fluid techniques to increase berberine solubility and bioavailability by reducing particle size using the GAS (Gas Anti-Solvent) antisolvent technique.

Results

Particle size was reduced to 6.34 μm (optimal condition with methanol at 20 mL/min CO₂ flow), with cumulative dissolution increased by 18% compared to raw material. FTIR confirmed preservation of functional groups, and increases in melting temperature and dissolution rate were observed. XRD analysis indicated potential formation of new polymorphic forms with ethanol treatment.

Conclusion

The GAS antisolvent technique proved effective for berberine micronization and enhancement of dissolution properties. The method achieved narrow particle size distribution and solvent-free products while maintaining structural integrity. This approach offers promising potential for improving berberine bioavailability and expanding its pharmaceutical applications.
  • Published in:ACS Omega,
  • Study Type:Experimental Study,
  • Source: 10.1021/acsomega.5c01675, PMID: 41210731
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