Tremblay C, Barza M, Fiore C, Szoka F
Antimicrob Agents Chemother. 1984 Aug;26(2):170-3. doi: 10.1128/AAC.26.2.170.
We developed a liposome-intercalated preparation of amphotericin B by using small, unilamellar vesicles 0.06 to 0.1 micron in diameter. In contrast to previously described liposomal preparations of amphotericin B, these vesicles have the advantage that they are small enough to be filter sterilized. We compared the efficacy of liposomal amphotericin B with that of the commercial drug given as an intravenous bolus every other day for 13 days (seven doses) in mice with disseminated candidiasis. Survival rates were similar for the two preparations at each dosage of amphotericin B; however, the highest survival rates occurred at dosages of liposomal amphotericin B which would be lethal to these animals if administered as the commercial drug. Viable colony counts of fungi in various organs, particularly the kidneys, tended to be lower with increasing dosage of the drug. However, some organisms persisted even after 13 days. These studies indicate that liposomal formulations of amphotericin B merit further investigation because of their improved therapeutic margins.
我们通过使用直径为0.06至0.1微米的小单层囊泡,开发了一种两性霉素B脂质体插层制剂。与先前描述的两性霉素B脂质体制剂相比,这些囊泡的优点是它们足够小,可以通过过滤进行灭菌。我们比较了脂质体两性霉素B与市售药物的疗效,在患有播散性念珠菌病的小鼠中,每隔一天静脉推注一次,持续13天(七剂)。在两性霉素B的每个剂量下,两种制剂的存活率相似;然而,脂质体两性霉素B的最高存活率出现在如果作为市售药物给药对这些动物致死的剂量下。随着药物剂量的增加,各个器官,特别是肾脏中的真菌活菌落计数往往会降低。然而,即使在13天后仍有一些微生物存活。这些研究表明,两性霉素B的脂质体制剂因其改善的治疗优势值得进一步研究。