Department of Pharmaceutics, Graduate School of Pharmaceutical Sciences, Hokkaido Pharmaceutical University, 7-1 Katsuraoka-cho, Otaru, Japan.
Drug Dev Ind Pharm. 2011 Apr;37(4):367-72. doi: 10.3109/03639045.2010.513389. Epub 2010 Sep 6.
The efficacy of aerosolization of ciprofloxacin (CPFX) incorporated into PEGylated liposomes (PEGylated CPFX-liposomes) for the treatment of respiratory infections was evaluated.
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.
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.
This study shows that PEGylated CPFX-liposomes are a useful aerosol-based pulmonary drug delivery system for the treatment of respiratory infections.
评估将环丙沙星（CPFX）包封于聚乙二醇化脂质体（PEGylated CPFX-脂质体）中用于治疗呼吸道感染的疗效。
制备粒径为 100nm 的 1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-n-[甲氧基（聚乙二醇）-2000]（PEGylated CPFX-脂质体），并在大鼠中考察了 PEGylated CPFX-脂质体雾化后在肺上皮衬液（ELF）中的药物分布特征。此外，通过药代动力学/药效学分析评价 PEGylated CPFX-脂质体在 ELF 中的抗菌作用。
PEGylated CPFX-脂质体雾化后 CPFX 从 ELF 中的消除率明显慢于未修饰脂质体（未修饰 CPFX-脂质体；粒径：100nm）中 CPFX 的消除率。根据药代动力学/药效学分析，PEGylated CPFX-脂质体对 ELF 中的致病微生物具有强大的抗菌作用。
本研究表明，PEGylated CPFX-脂质体是一种用于治疗呼吸道感染的有用的基于气雾剂的肺部药物递送系统。
