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

Berberine is a compound widely used in Chinese herbal medicine. It can potentially treat diabetes, cholesterol, and mental illnesses and has antimicrobial effects. However, its application is limited due to its low solubility in water, thus limiting its bioavailability. Micronization techniques are used to increase the surface area and improve the dissolution rate. The micronized particles were produced using the antisolvent GAS technique at a temperature of 35 °C and 80 bar. A solubility study with acetone, dichloromethane, ethanol, methanol, 1-butanol, and 1-propanol was carried out. Fourier-transform infrared spectroscopy analysis confirmed the preservation of functional groups. Additionally, a reduction in particle size to 6.34 μm was achieved, which contributed to an increase of up to 18% in cumulative dissolution. Furthermore, an increase in melting temperature and dissolution rate was observed. Thus, the antisolvent GAS technique proves to be an efficient approach for particle micronization and the consequent enhancement of dissolution properties.

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Publication Details

Journal
ACS Omega
Published
2025-10-22
DOI
https://doi.org/10.1021/acsomega.5c01675
Primary Topic
Berberine and alkaloids research
Type
article
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article

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

Gean Pablo S. Aguiar, Guilherme S.B. Sakata, Patrícia Viera de Oliveira, Marcelo Lanza et al.
ACS Omega
Berberine and alkaloids research
article

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

Gean Pablo S. Aguiar, Guilherme S.B. Sakata, Patrícia Viera de Oliveira, Marcelo Lanza, J. Vladimir Oliveira
article en

Abstract

Berberine is a compound widely used in Chinese herbal medicine. It can potentially treat diabetes, cholesterol, and mental illnesses and has antimicrobial effects. However, its application is limited due to its low solubility in water, thus limiting its bioavailability. Micronization techniques are used to increase the surface area and improve the dissolution rate. The micronized particles were produced using the antisolvent GAS technique at a temperature of 35 °C and 80 bar. A solubility study with acetone, dichloromethane, ethanol, methanol, 1-butanol, and 1-propanol was carried out. Fourier-transform infrared spectroscopy analysis confirmed the preservation of functional groups. Additionally, a reduction in particle size to 6.34 μm was achieved, which contributed to an increase of up to 18% in cumulative dissolution. Furthermore, an increase in melting temperature and dissolution rate was observed. Thus, the antisolvent GAS technique proves to be an efficient approach for particle micronization and the consequent enhancement of dissolution properties.

ACS OmegaVol. 10(43)
Community University of Chapecó Region - Unochapecó (BR), Universidade Federal de Santa Catarina (BR)
Openalex Percentile: Top 66%
Berberine and alkaloids research
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