Abstract

The enhancing effect of hydrophilic groups of phospholipids on the percutaneous penetration of indomethacin (IM) in vitro was examined in a Franz-type diffusion chamber using dorsal skin of guinea pigs. Phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylinositol (PI), phosphatidylserine (PS), phosphatidylglycerol (PG), phosphatidic acid (PA) and sphingomyelin (SM) were used as phospholipids. The enhancing effects of these phospholipids on the percutaneous penetration of IM through the skin were in the following order: PG > PE > PC > PS > PA > PI > control > SM. In the experiment of pretreatment with phospholipids, PC, PE and PG significantly enhanced the percutaneous penetration of IM. In the skin without stratum corneum, percutaneous penetration of IM was not significantly affected by PG, PE, PC or SM; however, it was slightly suppressed by SM. These results suggest that phospholipids have a direct influence on the lipid bilayer of the cell membrane in the stratum corneum and the enhancement of percutaneous penetration of IM by phospholipids is due to the alteration of permeability by the interaction of the cell membrane with phospholipids in the skin.

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