Sasaki H, Kishikawa M, Nakamura J, Shibasaki J
Faculty of Pharmaceutical Sciences, Nagasaki University, Japan.
J Pharmacobiodyn. 1990 Aug;13(8):468-74. doi: 10.1248/bpb1978.13.468.
Effect of pyrrolidone derivatives on lipid membrane and protein conformation has been assessed to obtain fundamental information about a mechanism of transdermal penetration enhancer. Their effects on a release of 6-carboxyfluorescein from liposome were examined. The lipophilic derivatives enhanced a release of dye and the enhancing effect showed a concentration dependency. Especially 1-lauryl-2-pyrrolidone showed the highest effect at the lowest concentration. The pyrrolidone derivatives also increased a hemolysis of rat erythrocytes. The derivatives slightly liberated SH group of keratin but did not change the electrophoresis pattern of keratin. 1-Methyl-2-pyrrolidone increased and retained a hydration of rat skin although 1-hexyl- and 1-lauryl-2-pyrrolidone showed no increase. These results suggest that the high enhancing effect of II, III and IX, as shown in the previous study, may be predominantly due to their interaction with skin lipid and their penetration behavior into the lipid.
已评估吡咯烷酮衍生物对脂质膜和蛋白质构象的影响，以获取有关透皮渗透促进剂作用机制的基础信息。研究了它们对脂质体中6-羧基荧光素释放的影响。亲脂性衍生物增强了染料的释放，且增强作用呈现浓度依赖性。特别是1-月桂基-2-吡咯烷酮在最低浓度时显示出最高效果。吡咯烷酮衍生物还增加了大鼠红细胞的溶血作用。这些衍生物使角蛋白的SH基团略有释放，但未改变角蛋白的电泳图谱。1-甲基-2-吡咯烷酮增加并保持了大鼠皮肤的水合作用，而1-己基-和1-月桂基-2-吡咯烷酮则未显示出增加。这些结果表明，如先前研究所示，II、III和IX的高增强作用可能主要归因于它们与皮肤脂质的相互作用及其向脂质中的渗透行为。
