RMP-7对两性霉素B脂质体跨血脑屏障能力的药效学研究  

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

作　　者：张小滨[1] 袁珊[2] 雷鹏程[2] 侯新朴[1] 

机构地区：[1]北京大学药学院物理药学教研室,北京100083 [2]北京大学第三临床医学院皮肤科,北京100083

出　　处：《药学学报》2004年第4期292-295,共4页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目 ( 30 1 71 1 1 4;2 9992 590 )

摘　　要：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 2h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 。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.

关 键 词：RMP-7 两性霉素B 脂质体 跨血脑 屏障能力 药效学 抗生素 

分 类 号：R978.1[医药卫生—药品]