Ergosterol (Ergo) and cholesterol contribute to performances of liposomes by increasing membrane packing density and physical stability. However, as these sterols can reduce membrane flexibility, they can lower skin permeability of liposomes. We synthesized ergosterol ester (Ergo-Est) containing unsaturated fatty acid different from Ergo in size and physical properties. In this work, we investigated effects of Ergo-Est and Ergo on physical properties of liposomes. We incorporated Ergo, Ergo-oleate (EO^18:1), Ergo-linoleate (EL^18:2), and Ergo-linolenate (ELn^18:3) into the liposomal membrane of egg phosphatidylcholine and soybean lecithin. Ergo-Est did not reduce membrane fluidity as much as Ergo. Nevertheless, Ergo-Est increased membrane packing density and physical stability of liposomes. EL^18:2 and ELn^18:3 almost maintained membrane flexibility and skin permeability of liposomes, while Ergo significantly reduced them. Skin permeation test demonstrated that EL^18:2 and ELn^18:3 liposomes permeated to the dermis, whereas Ergo liposome mostly remained in the stratum corneum. This is the first report to show that EL^18:2 and ELn^18:3 can be efficient sterol compounds for flexible liposome formulation.

麦角固醇 (Ergo) 和胆固醇通过增加膜堆积密度和物理稳定性来提高脂质体的性能。然而，由于这些甾醇会降低膜的柔韧性，因此它们会降低脂质体的皮肤渗透性。我们合成了麦角甾醇酯 (Ergo-Est)，其中含有与麦角甾醇大小和物理性质不同的不饱和脂肪酸。在这项工作中，我们研究了 Ergo-Est 和 Ergo 对脂质体物理性质的影响。我们合并了麦角、麦角-油酸酯 (EO ^18:1 )、麦角-亚油酸酯 (EL ^18:2 ) 和麦角-亚麻酸酯 (ELn ^18:3)进入卵磷脂酰胆碱和大豆卵磷脂的脂质体膜。Ergo-Est 不像 Ergo 那样降低膜流动性。然而，Ergo-Est 增加了脂质体的膜堆积密度和物理稳定性。EL ^18:2和 ELn ^18:3几乎保持了脂质体的膜柔韧性和皮肤渗透性，而 Ergo 显着降低了它们。皮肤渗透试验表明，EL ^18:2和 ELn ^18:3脂质体渗透到真皮，而 Ergo 脂质体主要留在角质层。这是第一份报告表明 EL ^18:2和 ELn ^18:3可以是用于柔性脂质体制剂的有效甾醇化合物。