Research on Membrane-Fluidity and Stratum Corneum Penetration of Liposomes Made of Phospholipid with Different Acyl Groups

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  • 異なるアシル基からなるリン脂質を用いたリポソームの微視的流動性とその角層浸透性に関する研究
  • コトナル アシルキ カラ ナル リン シシツ オ モチイタ リポソーム ノ ビシテキ リュウドウセイ ト ソノ カクソウ シントウセイ ニ カンスル ケンキュウ

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Abstract

The phospholipid is known to be safe and have superior tactile sensation, as well as to have the ability to improve the skin penetration of active ingredients, and it has been reported that the fact that the hydrophobic group of phospholipid is made of unsaturated fatty acid plays an important role in this process. However, the correlation between the membrane-fluidity of hydrophobic group and stratum corneum (SC) penetration has not been examined in detail. Therefore, in this study, we focused on the characteristics of phospholipids, and evaluated the correlation between membrane-fluidity and SC penetration. We also evaluated the interaction between liposomes and SC lipid liposome, and verified the mechanism of SC penetration. First, we created different types of liposomes: DPPC, whose acyl is made of saturated fatty acid; DOPC, which is made of unsaturated fatty acid; POPC, which has both saturated and unsaturated fatty acid in one molecule and a lipid component (DP+DO) which is mixture of DPPC and DOPC with molar ratio of 1: 1. As we examined the correlation between membrane-fluidity of the hydrophobic group and SC penetration of the water soluble component that coexists with membrane-fluidity, we found that POPC and DOPC, whose membrane-fluidity is high, have high SC penetration, and DPPC, whose membrane-fluidity is low, has low SC penetration. As we moved on to evaluating the influence that each phospholipid has on the membrane-fluidity of SC lipid liposome, correlation with the membrane-fluidity of the hydrophobic group of each phospholipid was indicated, and POPC showed the highest level of influence. These results suggest that as for SC penetration, even though unsaturated fatty acid of the phospholipid is a significant factor, the structure in which unsaturated and saturated fatty acid exist in the same molecule and stand alternately in membrane formation, like that of POPC, effectively changes the membrane-fluidity of SC lipid liposome, and accelerates SC penetration.

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