Paul M, Durand R, Fessi H, Rivollet D, Houin R, Astier A, Deniau M
Laboratoire de Pharmacotechnie, Service Pharmacie, CHU H. Mondor, Creteil, France.
Antimicrob Agents Chemother. 1997 Aug;41(8):1731-4. doi: 10.1128/AAC.41.8.1731.
The efficacy of a new liposomal formulation of amphotericin B was compared to that of amphotericin B deoxycholate (Fungizone) in a murine model of visceral leishmaniasis induced by Leishmania infantum. Median effective doses (ED50) were determined with two different strains: strain 1 was obtained from an untreated patient, and strain 2 was obtained from a patient who had received 12.5 g of amphotericin B over 3 years. BALB/c mice were infected intravenously on day 0 with promastigotes and then treated on days 14, 16, and 18 (strain 1) or on days 21, 23, and 25 (strain 2) with the liposomal formulation of amphotericin B (five doses were tested for each strain: 0.05, 0.1, 0.5, 0.8, and 3 mg/kg of body weight) or with conventional amphotericin B (four doses were tested for each strain: 0.05, 0.1, 0.5, and 0.8 mg/kg). Mice in the control group received normal saline solution. The liposomal amphotericin B formulation was about three times more active than the conventional drug against both strains. ED50 of the liposomal formulation were 0.054 (strain 1) and 0.194 (strain 2) mg/kg. ED50 of conventional amphotericin B were 0.171 (strain 1) and 0.406 (strain 2) mg/kg. Determination of drug tissular levels, 3 days after the last drug administration, showed a drug accumulation in hepatic and splenic tissues much higher after administration of liposomal amphotericin B than after conventional amphotericin B. A lack of toxicity was noted in all groups treated with the liposomal formulation.
在由婴儿利什曼原虫引起的内脏利什曼病小鼠模型中,将两性霉素B的一种新的脂质体制剂的疗效与两性霉素B脱氧胆酸盐(两性霉素B)进行了比较。用两种不同的菌株测定了半数有效剂量(ED50):菌株1取自一名未经治疗的患者,菌株2取自一名在3年期间接受了12.5g两性霉素B治疗的患者。在第0天,将BALB/c小鼠静脉注射前鞭毛体,然后在第14、16和18天(菌株1)或第21、23和25天(菌株2)用两性霉素B脂质体制剂(对每个菌株测试了五个剂量:0.05、0.1、0.5、0.8和3mg/kg体重)或传统两性霉素B(对每个菌株测试了四个剂量:0.05、0.1、0.5和0.8mg/kg)进行治疗。对照组的小鼠接受生理盐水溶液。两性霉素B脂质体制剂对两种菌株的活性比传统药物高约三倍。脂质体制剂的ED50分别为0.054(菌株1)和0.194(菌株2)mg/kg。传统两性霉素B的ED50分别为0.171(菌株1)和0.406(菌株2)mg/kg。在最后一次给药后3天测定药物组织水平,结果显示给两性霉素B脂质体制剂后,肝脏和脾脏组织中的药物蓄积量比给传统两性霉素B后高得多。在用脂质体制剂治疗的所有组中均未观察到毒性。