Liposome-skin interactions and their effects on the skin permeation of drugs.
The aim of the study was to evaluate the interaction of phospholipid liposomes with skin and stratum corneum lipid liposomes (SCLLs). The influence of phospholipid liposomes on the skin permeability of model drugs was also studied. The transdermal flux of the drugs applied in various phospholipid containing formulations through human epidermis was studied in diffusion chambers. Liposomes in water solutions did not enhance the skin permeability of the drugs, but when ethanol (32% w/v) was present in the donor with EPC (egg yolk lecithin), permeabilities of some model drugs were substantially increased. Confocal microscopy studies revealed that EPC do not penetrate into the skin from water solutions, while from ethanol solutions, EPC penetrates deeply into the stratum corneum. Also, resonance energy transfer between different liposome compositions and the release of calcein from SCLLs showed that interactions between phospholipid liposomes and SCLLs increased with increasing ethanol concentration in the liposome solutions.
Kirjavainen
M
M
Department of Pharmaceutics, University of Kuopio, P.O. Box 1627, FIN-70211 Kuopio, Finland.mhakkara@uku.fi
Urtti
A
A
Valjakka-Koskela
R
R
Kiesvaara
J
J
Mönkkönen
J
J
D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D004337:Drug Carriers / Q000494:pharmacology; D004735:Energy Transfer; D005452:Fluoresceins / Q000493:pharmacokinetics; D005456:Fluorescent Dyes / Q000493:pharmacokinetics; D006801:Humans; D066298:In Vitro Techniques; D008081:Liposomes / Q000494:pharmacology*; D018613:Microscopy, Confocal; D004364:Pharmaceutical Preparations / Q000378:metabolism; D010743:Phospholipids; D011433:Propranolol / Q000008:administration & dosage / Q000493:pharmacokinetics; D012869:Skin Absorption / Q000187:drug effects*; D013015:Sotalol / Q000008:administration & dosage / Q000493:pharmacokinetics