Use of Liposomes on Modification of Stratum Corneum Lipids and Enhancement of Transdermal Drug Permeation

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With the aim of efficient delivery of lipids and lipid analogs to skin, we studied the stability of cationic liposomes containing double-chained cationic surfactants, the interaction of the liposomes with erythrocyte membrane as well as that with skin. Dimethyldipalmitylammonium formed stable liposomes in the presence of phosphatidylcholines with unsaturated acy1 chains, whereas 1,2-dioleoyl-3-trimethylammonium propane formed the stable liposomes even in the presence of phosphatidylcholines with saturated acy1 chains. These cationic liposomes induced aggregation and fusion of the erythrocytes. By using such interaction of the liposomes with biological membranes we tried to deliver ceramide to lipid deficient skin. We confirmed that ceramide and dimethyl-dipalmitylammonium formed stable bilayer vesicles in the presence of cholesterol at a molar ratio of 1:1:1. The addition of the cationic liposomes to 80% ethanol-treated delipidized guinea pig dorsal skin slightly recovered the rigidity of the stratum corneum lipid lamella and had a tendency to recover its barrier function. We furthermore found the enhanced incorporation of retinoic acid using cationic liposomes. Through these findings we clarified the usefulness of the cationic liposomes to efficient delivery of lipids and lipid analogs to skin.