Hossain M A, Maesaki S, Kakeya H, Noda T, Yanagihara K, Sasaki E, Hirakata Y, Tomono K, Tashiro T, Kohno S
Second Department of Internal Medicine, Nagasaki University School of Medicine, Japan.
Antimicrob Agents Chemother. 1998 Jul;42(7):1722-5. doi: 10.1128/AAC.42.7.1722.
In vitro and in vivo efficacies of NS-718, a lipid nanosphere-encapsulated amphotericin B (AMPH-B), have been studied. Of the tested AMPH-B formulations, NS-718 had the lowest MIC for Cryptococcus neoformans. In a murine model, low-dose therapy (0.8 mg/kg of body weight) with NS-718 showed higher efficacy than that with AmBisome. High-dose therapy (2.0 mg/kg) with NS-718 was much more effective than those with Fungizone and AmBisome. In mice treated with a high dose of NS-718, only a few yeast cells had grown in lung by 7 days after inoculation. A pharmacokinetic study showed higher concentrations of AMPH-B in lung following administration of NS-718 than after administration of AmBisome. Our results indicated that NS-718, a new AMPH-B formulation, is a promising antifungal agent for treatment of pulmonary cryptococcosis and could be the most effective antifungal agent against C. neoformans infections.
已对脂质纳米球包裹的两性霉素B(AMPH - B)制剂NS - 718的体外和体内疗效进行了研究。在所测试的AMPH - B制剂中,NS - 718对新型隐球菌的最低抑菌浓度(MIC)最低。在小鼠模型中,NS - 718低剂量治疗(0.8毫克/千克体重)比安必素治疗显示出更高的疗效。NS - 718高剂量治疗(2.0毫克/千克)比两性霉素B和安必素更有效。在接受高剂量NS - 718治疗的小鼠中,接种后7天肺部仅有少数酵母细胞生长。一项药代动力学研究表明,给予NS - 718后肺部AMPH - B的浓度高于给予安必素后。我们的结果表明,新型AMPH - B制剂NS - 718是治疗肺隐球菌病的一种有前景的抗真菌药物,可能是对抗新型隐球菌感染最有效的抗真菌药物。