目的：：制备具有靶向性抗耐药菌作用的左氧氟沙星脂质体,并考察其体外抗菌活性。方法：采用硫酸铵梯度法,用Ts修饰脂质体膜,制备具双重杀菌机制的靶向左氧氟沙星脂质体,考察其表征及包封率。比较游离左氧氟沙星、左氧氟沙星与 Ts 联合、非靶向及靶向左氧氟沙星脂质体对耐药菌株的最小抑菌浓度( MIC)及对肺炎克雷伯标准菌株的时间杀菌活性,并分析协同效应。结果：靶向左氧氟沙星脂质体包封率(75.26±1.35)%,粒径(152.5±3.2)nm,zeta电位+20.68±1.72,多分散性0.149±0.02,1个月内稳定性较好,其MIC均低于其他剂型,FIC≤0.5,显示协同效应；在同一时间内抑菌数量最多,时间杀菌效果显著。结论：相对游离剂型和非靶向脂质体,靶向左氧氟沙星脂质体对耐药菌具备更强的抗菌活性。%Objective:To prepare levofloxacin liposome with targeting antagonizing drug-resistance bacteria effect and observe its antimicrobial activity in vitro. Methods: Ammonium sulfate gradient method and modify the liposome membrane with Ts were used to produce targeting levofloxacin liposome with double antibacterial mechanisms. MIC ( minimum inhibitory Concentration) and time-bactericidal activity to pneumonia klebsiella were compared among free levofloxacin, levofloxacin combined with Ts, non-targeting and targeting levofloxacin liposome and analysis synergistic effect. Results: The encapsulation efficiency of targeting levofloxacin liposome was (75. 26 ± 1. 35)%, partical size was(152. 5 ± 3. 2) nm, Zeta potential was+20. 68 ± 1. 72, and polydispersity was 0. 149 ± 0. 02. Liposome was stable for one month. The MIC was lower than other forms. FIC≤0. 5 showed synergistic effect. During the same time, it inhibited most bacteria with outstanding time-bactericidal activity. Conclusion: Comparing with free and non- targeting liposome, targeting levofloxacin liposome has greater bactericidal activity to drug-resistance bacteria.
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