title: Efficient drug delivery to lung epithelial lining fluid by aerosolization of ciprofloxacin incorporated into PEGylated liposomes for treatment of respiratory infections.
abstract: OBJECTIVE
  The efficacy of aerosolization of ciprofloxacin (CPFX) incorporated into PEGylated liposomes (PEGylated CPFX-liposomes) for the treatment of respiratory infections was evaluated.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  This study shows that PEGylated CPFX-liposomes are a useful aerosol-based pulmonary drug delivery system for the treatment of respiratory infections.
authors.affiliation: Department of Pharmaceutics, Graduate School of Pharmaceutical Sciences, Hokkaido Pharmaceutical University, 7-1 Katsuraoka-cho, Otaru, Japan. s-chono@hokuyakudai.ac.jp
authors.forename: Sumio
authors.initials: S
authors.lastname: Chono
authors.forename: Hirokazu
authors.initials: H
authors.lastname: Suzuki
authors.forename: Kohei
authors.initials: K
authors.lastname: Togami
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Morimoto
mesh_terms: D000336:Aerosols / Q000737:chemistry; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage*; D019540:Area Under Curve; D002939:Ciprofloxacin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D004848:Epithelium / Q000378:metabolism; D007770:L-Lactate Dehydrogenase / Q000032:analysis; D008081:Liposomes / Q000737:chemistry; D008168:Lung / Q000378:metabolism*; D008297:Male; D011092:Polyethylene Glycols / Q000008:administration & dosage; D051381:Rats; D017207:Rats, Sprague-Dawley; D012141:Respiratory Tract Infections / Q000188:drug therapy*
chemical_list: D000336:Aerosols; D000890:Anti-Infective Agents; D008081:Liposomes; D011092:Polyethylene Glycols; D002939:Ciprofloxacin; D007770:L-Lactate Dehydrogenase