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Volume 117
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Micronization of lopinavir using solution-enhanced dispersion by supercritical CO2
Lan Fang a *, Jing Zhang b, Fukang Wang c, Jianhua Wang a, Yan Huo a, Zhiyong Li a, Xiaomei Mao a, Mengting Qian a, Zhiqun Xu a *
a Suzhou Chien-shiung Institute of Technology, Taicang, 215411, China
b Department of Pharmaceutical Engineering, School of Engineering, China Pharmaceutical University, Nanjing, 211198, China
c Shanghai Advanced Research Institute, Chinese Academy of Sciences, Shanghai, 201210, China
10.1016/j.partic.2026.06.043
Volume 117, October 2026, Pages 1-7
Received 13 April 2026, Revised 28 June 2026, Accepted 30 June 2026, Available online 15 July 2026, Version of Record 20 July 2026.
E-mail: 9265@csit.edu.cn; 9279@csit.edu.cn
Highlights

• Lopinavir was successfully micronized by SEDS with supercritical CO2, achieving significant particle size reduction and high yield.

• The SEDS process retained the chemical structure and crystalline form of lopinavir with solvent residues meeting ICH standards.

• The micronized product showed greatly improved in vitro dissolution compared with the raw drug.


Abstract

Lopinavir (LPV) is a key antiviral drug limited in clinical application by its poor water solubility. This study employed solution-enhanced dispersion by supercritical CO2 (SEDS) technology for LPV micronization, and optimized four core process parameters via orthogonal experimental design. Under optimal conditions (15 MPa, 35 °C, 2 mg/mL, 1.2 mL/min), the mean particle size of LPV was reduced from 80.0 μm to 6.6 μm with a micronization yield of 82.5%. Characterizations verified that LPV retained its Type I crystalline form and chemical structure after processing, with residual solvents well below ICH limits. The in vitro dissolution performance was significantly enhanced, reaching 74.0% at 96 h versus 25.1% for raw LPV. This study confirms that SEDS is an efficient green approach for LPV micronization. It effectively improves the drug dissolution property while preserving structural and crystalline integrity, providing a feasible strategy for the formulation development of poorly water-soluble drugs.

Graphical abstract
Keywords
Lopinavir; Supercritical fluid; SEDS; CO2
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