RMP-7对两性霉素B脂质体跨血脑屏障能力的药效学研究RMP-7对两性霉素B脂质体跨血脑屏障能力的药效学研究

目的研究两性霉素B脑靶向脂质体对小鼠脑膜炎的治疗作用。方法用薄膜超声法制备两性霉素B脂质体和两性霉素B脑靶向脂质体,测定其包封率和浓度;建立小鼠的脑膜炎模型,研究了两性霉素B脂质体的疗效。结果两性霉素B脂质体的包封率为(93.3±1.8)%;脑内注射白色念珠球菌2 h使小鼠形成脑膜炎模型;将两性霉素B制成脑靶向脂质体,能显著延长脑膜炎小鼠的生存期。结论与普通两性霉素B脂质体相比,两性霉素B脑靶向脂质体能显著提高对小鼠脑膜炎的治疗作用,使小鼠的存活期延长一倍。

Therapeutic efficiency of amphotericin B liposome modified by RMP-7 to transport drug across blood brain barrier

AimTo study the therapeutic efficiency of amphotericin B liposome (AmB-L) targeting to the brain in mice with meningitis. MethodsAmphotericin B liposome targeting to the brain were prepared by film-sonication method. Their concentration and encapsulation percentage were determined. The Candida albicans was injected into the brain of BALB/c mice and the meningitis model was set up. Then the therapeutic efficiency of amphotericin B liposome targeting to the brain was studied. ResultsThe encapsulation percentage of amphotericin B liposome was 93 3%. The meningitis model was set up after the Candida albicans was injected into the brain of BALB/c mice for 2 h. The therapeutic efficiency was increased after conjugating RMP-7 (the commercial nama is Cereport) to the surface of amphotericin B liposome. ConclusionThe therapeutic efficiency of Amphotericin B liposome targeting to the brain in the mice with meningitis was better than that of the common amphotericin B liposome and the life of the mice in AmB-L-PEG-RMP-7 group was longer than that of the mice in AmB-L-PEG group and AmB-L-PEG RMP-7 group.