Hiemenz J W, Walsh T J
H. Lee Moffitt Cancer Center, University of South Florida, Tampa 33612, USA.
Clin Infect Dis. 1996 May;22 Suppl 2:S133-44. doi: 10.1093/clinids/22.supplement_2.s133.
Three lipid formulations of amphotericin B are now either marketed for clinical use or undergoing further study before they can be approved in various countries worldwide. Amphotericin B lipid complex (ABLC; Abelcet, Liposome Company, Princeton, NJ) is a concentration of ribbonlike structures of a bilayered membrane formed by combining a 7:3 molar ratio of dimyristoyl phosphatidylcholine and dimyristoyl phosphatidylglycerol with amphotericin B. Amphotericin B colloidal dispersion (ABCD; Amphocii, Sequus Pharmaceuticals, Menlo Park, CA) is composed of disklike structures of cholesteryl sulfate complexed with amphotericin B. AmBisome (Nexstar, San Dimas, CA), the only true liposomal amphotericin B, consists of small unilamellar vesicles made up of a bilayer membrane of hydrogenated soy phosphatidylcholine and distearoylphosphatidylglycerol stabilized with cholesterol in a 2:0.8:1 ratio combined with amphotericin B. All of the preparations appear to be preferentially accumulated in organs of the reticuloendothelial system, as opposed to the kidney. In vivo animal models as well as current clinical experience suggest that use of these formulations results in overall improvement in the therapeutic index. Patients with life-threatening mycosis for whom therapy has failed or who are intolerant to therapy with amphotericin B deoxycholate have been successfully treated with these formulations. However, further study is warranted to help clarify the usefulness of each of the lipid formulations as first-line therapy for documented or suspected invasive fungal infections.
两性霉素B的三种脂质制剂目前要么已上市用于临床，要么正在进行进一步研究，之后才能在世界各国获批。两性霉素B脂质复合物（ABLC；Abelcet，脂质体公司，新泽西州普林斯顿）是一种双层膜的带状结构聚集体，由二肉豆蔻酰磷脂酰胆碱和二肉豆蔻酰磷脂酰甘油按7:3的摩尔比与两性霉素B结合形成。两性霉素B胶体分散液（ABCD；Amphocii，Sequus制药公司Menlo Park，加利福尼亚州）由与两性霉素B复合的硫酸胆固醇盘状结构组成。安必素（Nexstar，加利福尼亚州圣迪马斯）是唯一真正的脂质体两性霉素B，由小单层囊泡组成，其双层膜由氢化大豆磷脂酰胆碱和二硬脂酰磷脂酰甘油组成，并以2:0.8:1的比例与胆固醇稳定结合，再与两性霉素B结合。所有这些制剂似乎都优先在网状内皮系统的器官中蓄积，而不是在肾脏中。体内动物模型以及当前的临床经验表明，使用这些制剂可使治疗指数总体得到改善。对于治疗失败或对两性霉素B脱氧胆酸盐治疗不耐受的危及生命的真菌病患者，使用这些制剂已成功治愈。然而，有必要进一步研究，以帮助阐明每种脂质制剂作为已记录或疑似侵袭性真菌感染一线治疗方法的有效性。
