Journal
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 37, Issue 4, Pages 367-372Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/03639045.2010.513389
Keywords
Aerosol-based pulmonary drug delivery system; ciprofloxacin; lung epithelial lining fluid; PEGylated liposomes; respiratory infections
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Funding
- Japan Society for the Promotion of Science (JSPS) [20590039]
- Japan Science and Technology Agency (JST)
- Northern Advancement Center for Science & Technology (NOASTEC, Sapporo, Japan)
- Akiyama Life Science Foundation (Sapporo, Japan)
- Grants-in-Aid for Scientific Research [20590039] Funding Source: KAKEN
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Purpose: The efficacy of aerosolization of ciprofloxacin (CPFX) incorporated into PEGylated liposomes (PEGylated CPFX-liposomes) for the treatment of respiratory infections was evaluated. Method: PEGylated CPFX-liposomes with 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-n-[methoxy(polyethylene glycol)2000] (particle size: 100 nm) were prepared, and the drug distribution characteristics in lung epithelial lining fluid (ELF) following aerosolization of PEGylated CPFX-liposomes were examined in rats. Furthermore, the antibacterial effects of PEGylated CPFX-liposomes in ELF were evaluated by pharmacokinetic/pharmacodynamic analysis. Results: The elimination rate of CPFX from ELF following aerosolization of PEGylated CPFX-liposomes was significantly slower than that of CPFX incorporated into unmodified liposomes (unmodified CPFX-liposomes; particle size: 100 nm). According to pharmacokinetic/pharmacodynamic analysis, the PEGylated CPFX-liposomes exhibited potent antibacterial effects against pathogenic microorganisms in ELF. Conclusion: This study shows that PEGylated CPFX-liposomes are a useful aerosol-based pulmonary drug delivery system for the treatment of respiratory infections.
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