Ciprofloxacin nanocrystals and N-acetylcysteine co-solidified powders for pulmonary drug delivery: development and in vitro and in vivo characterization

This study evaluated the feasibility of ciprofloxacin nanocrystals dry powder inhalations (DPIs) co-delivered with N-acetylcysteine (NAC) to improve the drug permeability and pulmonary bioavailability. The NAC could be reducing the viscosity of the sputum and causing it to liquefy, by breaks DNA fib...

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Bibliographic Details
Published in:Journal of nanoparticle research : an interdisciplinary forum for nanoscale science and technology 2022-02, Vol.24 (2), Article 41
Main Authors: Guan, Wenhao, Liu, Yanchao, Ding, Shuaijie, Wang, Yancai
Format: Article
Language:English
Subjects:
Acetylcysteine
Aerosols
Antibiotics
Bioavailability
Characterization and Evaluation of Materials
Chemistry and Materials Science
Ciprofloxacin
Crystals
DNA damage
Drug delivery
Drug delivery systems
Feasibility studies
Fibers
Freeze drying
In vivo methods and tests
Inorganic Chemistry
Lactose
Lasers
Materials Science
Nanocrystals
Nanotechnology
Optical Devices
Optics
Particle size distribution
Permeability
Photonics
Physical Chemistry
Polyethylene glycol
Powder
Research Paper
Sputum
Stability analysis
Synergistic effect
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Summary:This study evaluated the feasibility of ciprofloxacin nanocrystals dry powder inhalations (DPIs) co-delivered with N-acetylcysteine (NAC) to improve the drug permeability and pulmonary bioavailability. The NAC could be reducing the viscosity of the sputum and causing it to liquefy, by breaks DNA fibers in sputum and purulent sputum. The ciprofloxacin nanocrystals, stabilized by 1, 2-distearoyl-sn-glycero-3-phosphoethanolamine grafted N-[methoxy (polyethylene glycols)-2000] (DSPE-mPEG 2000 ), was prepared by anti-solvent precipitation technology. The powder contained ciprofloxacin nanocrystals and N-acetyl-cysteine was obtained as a result of freeze-drying and spray-drying, respectively. The powder was coupled with inhaled lactose and the DPI of ciprofloxacin nanocrystals/NAC co-delivery system was obtained. The in vitro characteristics, including particle size and distribution, morphology, crystalline state, stability, flowability, aerosol performance, and in vivo image were evaluated. The spray-dried DPI of ciprofloxacin nanocrystals/NAC co-delivery system exhibited stratified in vitro and in vivo aerosol performance. This study demonstrated that spray-dried DPI system with a synergistic effect and meanwhile a better flowability is desirable for enhanced pulmonary drug delivery without severe lung injury.
ISSN:1388-0764
1572-896X
DOI:10.1007/s11051-022-05427-1