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Inhalable Nanocomposite Microparticles with Enhanced Dissolution and Superior Aerosol Performance
Chune Zhu1,2, Jianting Chen2, Shihui Yu2
1School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, 280 Waihuan East Road, Guangzhou 510006, China.
Molecular Pharmaceutics
|July 10, 2020
Summary
This study developed inhalable nanoparticles combining colistin and ivacaftor to treat cystic fibrosis lung infections. The novel formulation improves drug dissolution and aerosol performance for simultaneous treatment.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Nanotechnology
Background:
- Colistin (Col) and ivacaftor (Iva) show synergistic effects against Pseudomonas aeruginosa.
- Cystic fibrosis (CF) requires treatments for both the disease and lung infections.
Purpose of the Study:
- Develop dry powder inhaler (DPI) formulations for co-delivery of Col and Iva.
- Enable simultaneous treatment of CF and lung infections.
Main Methods:
- Encapsulate water-insoluble Iva into bovine serum albumin (BSA) nanoparticles (Iva-BSA-NPs).
- Produce inhalable composite microparticles via spray-freeze-drying using Col as matrix and l-leucine as aerosol enhancer.
- Characterize morphology, amorphous state, and aerosol performance (FPF).
Main Results:
- Optimal formulation achieved high fine particle fractions (FPF): 73.8% for Col, 80.9% for Iva.
- Iva-BSA-NPs remained amorphous, enhancing solubility 66-fold.
- Rapid in vitro release of both drugs within 3 hours, significantly faster for Iva compared to physical mixtures.
Conclusions:
- Developed novel inhalable nanocomposite microparticles for co-delivery of Col and Iva.
- Achieved reduced excipient use, improved dissolution of water-insoluble Iva, and superior aerosol performance.
- Demonstrated potential for simultaneous treatment of CF and lung infections.
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