Lopez-Berestein G, Mehta R, Hopfer R, Mehta K, Hersh E M, Juliano R
Cancer Drug Deliv. 1983;1(1):37-42. doi: 10.1089/cdd.1983.1.37.
Incorporation of amphotericin B (AMP-B) into phospholipid vesicles (liposomes) has been shown previously to decrease AMP-B toxicity while retaining the antifungal efficacy of the drug. In this report, the role of sterols in the formulation of liposomes as well as in their effectiveness in the treatment of murine candidiasis have been investigated. The presence of ergosterol or cholesterol at different lipid ratios did not augment the encapsulation efficiency of AMP-B as compared with vesicles containing phospholipids alone. There was no significant difference in the survival time of mice infected with Candida albicans treated with sterol-containing vesicles compared with those treated with sterol-free vesicles. These findings suggest that the sterol-free liposomes might be of advantage for delivering AMP-B because of its simple formulation, lack of toxicity, and ease of preparation.
先前已表明,将两性霉素B(AMP - B)掺入磷脂囊泡(脂质体)中可降低AMP - B的毒性,同时保留该药物的抗真菌功效。在本报告中,研究了甾醇在脂质体制备中的作用以及它们在治疗小鼠念珠菌病中的有效性。与仅含磷脂的囊泡相比,不同脂质比例下麦角固醇或胆固醇的存在并未提高AMP - B的包封效率。用含甾醇囊泡治疗的白色念珠菌感染小鼠的存活时间与用无甾醇囊泡治疗的小鼠相比,没有显著差异。这些发现表明,无甾醇脂质体可能有利于递送AMP - B,因为其配方简单、无毒且易于制备。