Mehta R T, Hopfer R L, McQueen T, Juliano R L, Lopez-Berestein G
Department of Clinical Immunology, University of Texas M.D. Anderson Hospital and Tumor Institute, Houston.
Antimicrob Agents Chemother. 1987 Dec;31(12):1901-3. doi: 10.1128/AAC.31.12.1901.
The therapeutic activity of nystatin (NYS) incorporated in multilamellar liposomes (L-NYS) was studied in vivo. Hale-Stoner mice injected intravenously with various doses of L-NYS and free NYS showed a significant reduction in toxicity of NYS after the NYS was incorporated into liposomes (maximal tolerated doses, 16 and 4 mg/kg of body weight, respectively). The maximal tolerated dose of free NYS had no effect in the treatment of mice infected with Candida albicans, whereas L-NYS at an equivalent dose improved the survival of mice. A marked increase in survival was observed when L-NYS was administered in higher and multiple doses (total doses up to 80 mg/kg). Liposome encapsulation thus provided a means for intravenous administration of NYS, reducing its toxicity and making it an active systemic antifungal agent.
研究了多层脂质体包裹的制霉菌素（L-NYS）在体内的治疗活性。给Hale-Stoner小鼠静脉注射不同剂量的L-NYS和游离制霉菌素（NYS），结果显示将NYS包裹于脂质体后其毒性显著降低（最大耐受剂量分别为16和4 mg/kg体重）。游离NYS的最大耐受剂量对感染白色念珠菌的小鼠治疗无效，而同等剂量的L-NYS可提高小鼠的存活率。当给予更高剂量和多次剂量（总剂量高达80 mg/kg）的L-NYS时，观察到存活率显著提高。因此，脂质体包封为NYS的静脉给药提供了一种方法，降低了其毒性并使其成为一种有效的全身性抗真菌剂。
