Department of Pharmaceutical Technology and Drug Delivery System Excellence Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkla 90112, Thailand.
J Pharm Sci. 2011 May;100(5):1727-35. doi: 10.1002/jps.22398. Epub 2010 Nov 24.
The antifungal activity of amphotericin B (AmB) incorporated in three cholesteryl carbonate esters (CCEs), sodium cholesteryl carbonate, cholesteryl palmityl carbonate, and dicholesteryl carbonate, was examined to assess their potential for use in a dry powder aerosol. Formulations containing dissolved AmB were stable for 6 months. The particle size varied inversely with liquid crystalline content with observed mass median aerodynamic diameters ranging from 4 to 8 μ m. This was consistent with the visual appearance of the liquid crystals as being low density and free flowing at room temperature. When dispersed in water, the presence of the CCE reduced the rate and extent of AmB release, consistent with the estimated liquid crystal/water partition coefficient. Nevertheless, the rate of AmB release was always sufficient to kill the fungus as established with bioactivity studies. AmB formulated with CCE as a dry powder appears to be promising for use in treating lung fungal infections.
将两性霉素 B（AmB）掺入三种胆甾醇碳酸酯（CCE）中，即胆甾醇碳酸酯钠、胆甾醇棕榈酸酯碳酸酯和二胆甾醇碳酸酯，以评估它们在干粉气溶胶中的潜在用途。含有溶解的 AmB 的制剂在 6 个月内稳定。颗粒大小与液晶含量成反比，观察到的质量中值空气动力学直径范围为 4 至 8 微米。这与液晶在室温下的低密度和自由流动的视觉外观一致。当分散在水中时，CCE 的存在降低了 AmB 的释放速度和程度，这与估计的液晶/水分配系数一致。然而，AmB 的释放速度始终足以杀死真菌，这是通过生物活性研究确定的。以 CCE 为赋形剂的 AmB 干粉似乎有望用于治疗肺部真菌感染。
