靶向左氧氟沙星脂质体的制备及其抗耐药菌作用的研究  

Study on targeting levofloxacin liposome against dug-resistance bacteria and its preparation

作　　者：樊菊香 吴国球[2] 严雪娇[1] 薛秀雷 曲青蓉 高维[1] 

机构地区：[1]东南大学医学院,江苏南京210009 [2]东南大学附属中大医院检验科,江苏南京210009

出　　处：《东南大学学报（医学版）》2015年第1期27-31,共5页Journal of Southeast University(Medical Science Edition)

基　　金：国家自然科学基金资助项目(81271636);江苏省自然科学基金资助项目(BK2009274)

摘　　要：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.＆nbsp;Conclusion： Comparing with free and non- targeting liposome, targeting levofloxacin liposome has greater bactericidal activity to drug-resistance bacteria.

关 键 词：抗菌肽 左氧氟沙星 脂质体 耐药菌 

分 类 号：R918[医药卫生—药学] R978.19