Effects of liposome size on penetration of dl-tocopherol acetate into skin.
Liposomes were prepared from hydrogenated lecithin (H-PC) by sonication (S) or injection (I) of H-PC dissolved in ethanol containing dl-tocopherol acetate (VEA). The effects of liposomes on the dermal absorption of VEA were studied. The particle diameter of S-liposomes was smaller than that of I-liposomes. The penetration of liposomal H-PC into the skin was much higher for S-liposomes than for I-liposomes 30 min after application to the arms of healthy human volunteers and also to hairless rat back skin. The penetration of 14C-VEA into hairless rat back skin was higher from the liposomes than from free VEA, and the 14C-VEA penetration was higher from S-liposomes than from I-liposomes. 3H-Dipalmitoylphosphatidylcholine and 14C-VEA, which had been entrapped in liposomes, were not detected in plasma. H-PC inhibited the peroxidation of skin lipids. H-PC enhanced the penetration of VEA into the skin, but the degree of enhancement depended on the size of the liposomes, indicating that this liposomal characteristic was an important factor in dermal absorption and/or penetration.
Natsuki
R
R
Faculty of Pharmaceutical Sciences, Setsunan University, Hirakata, Japan.
Morita
Y
Y
Osawa
S
S
Takeda
Y
Y
D015060:1,2-Dipalmitoylphosphatidylcholine / Q000008:administration & dosage; D000279:Administration, Cutaneous; D000328:Adult; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage*; D004337:Drug Carriers; D006801:Humans; D015227:Lipid Peroxidation / Q000187:drug effects; D008081:Liposomes / Q000737:chemistry*; D008297:Male; D010316:Particle Size; D010713:Phosphatidylcholines; D051381:Rats; D012869:Skin Absorption; D013010:Sonication; D024505:Tocopherols; D014810:Vitamin E / Q000008:administration & dosage / Q000031:analogs & derivatives*; D024502:alpha-Tocopherol / Q000031:analogs & derivatives*
D000975:Antioxidants; D004337:Drug Carriers; D008081:Liposomes; D010713:Phosphatidylcholines; D014810:Vitamin E; D015060:1,2-Dipalmitoylphosphatidylcholine; D024502:alpha-Tocopherol; D024505:Tocopherols