Conley J, Yang H, Wilson T, Blasetti K, Di Ninno V, Schnell G, Wong J P
SciLab Consulting Inc., Ralston, Alberta, Canada.
Antimicrob Agents Chemother. 1997 Jun;41(6):1288-92. doi: 10.1128/AAC.41.6.1288.
The aerosol delivery of liposome-encapsulated ciprofloxacin by using 12 commercially available jet nebulizers was evaluated in this study. Aerosol particles containing liposome-encapsulated ciprofloxacin generated by the nebulizers were analyzed with a laser aerodynamic particle sizer. Mean mass aerodynamic diameters (MMADs) and geometric standard deviations (GSDs) were determined, and the drug contents of the sampling filters from each run onto which aerosolized liposome-encapsulated ciprofloxacin had been deposited were analyzed spectrophotometrically. The aerosol particles of liposome-encapsulated ciprofloxacin generated by these nebulizers ranged from 1.94 to 3.5 microm, with GSDs ranging from 1.51 to 1.84 microm. The drug contents of the sampling filters exposed for 1 min to aerosolized liposome-encapsulated ciprofloxacin range from 12.7 to 40.5 microg/ml (0.06 to 0.2 mg/filter). By using the nebulizer selected on the basis of most desirable MMADs, particle counts, and drug deposition, aerosolized liposome-encapsulated ciprofloxacin was used for the treatment of mice infected with 10 times the 50% lethal dose of Francisella tularensis. All mice treated with aerosolized liposome-encapsulated ciprofloxacin survived the infection, while all ciprofloxacin-treated or untreated control mice succumbed to the infection (P < 0.001). These results suggest that aerosol delivery of liposome-encapsulated ciprofloxacin to the lower respiratory tract is feasible and that it may provide an effective therapy for the treatment of respiratory tract infections.
本研究评估了使用12种市售喷射雾化器进行脂质体包裹环丙沙星的气溶胶给药情况。用激光空气动力学粒径分析仪分析雾化器产生的含有脂质体包裹环丙沙星的气溶胶颗粒。测定平均质量空气动力学直径（MMAD）和几何标准差（GSD），并对每次运行后沉积有雾化脂质体包裹环丙沙星的采样滤器的药物含量进行分光光度分析。这些雾化器产生的脂质体包裹环丙沙星的气溶胶颗粒大小在1.94至3.5微米之间，GSD在1.51至1.84微米之间。暴露于雾化脂质体包裹环丙沙星1分钟的采样滤器的药物含量范围为12.7至40.5微克/毫升（0.06至0.2毫克/滤器）。通过使用基于最理想的MMAD、颗粒计数和药物沉积情况选择的雾化器，将雾化脂质体包裹环丙沙星用于治疗感染了10倍50%致死剂量土拉热弗朗西斯菌的小鼠。所有接受雾化脂质体包裹环丙沙星治疗的小鼠在感染后存活，而所有接受环丙沙星治疗或未治疗的对照小鼠均死于感染（P<0.001）。这些结果表明，将脂质体包裹环丙沙星气溶胶递送至下呼吸道是可行的，并且可能为治疗呼吸道感染提供一种有效的疗法。
