title: Interaction of liposome formulations with human skin in vitro.
abstract: The interaction of liposome formulations consisting of Phospholipon 80 and sphingomyelin with human skin was investigated. These formulations were shown previously to have a composition-dependent effect on the penetration of Heparin into the skin. Fluorescence labelled phosphatidylethanolamine (PE-NBD) was incorporated in the liposomes and the depth in which the fluorescent phospholipid label enters into epidermal membrane and full thickness skin was studied by confocal laser scanning microscopy (CLSM). Confocal sections parallel to the surface of the skin were recorded in heat separated epidermis. An even distribution of phospholipid in the lipid matrix of the stratum corneum surrounding the corneocytes was observed with Phospholipon 80 but not when sphingomyelin was included in the formulation. The addition of Heparin which formed a coating around the liposomes, caused a strong localization of fluorescence within the epidermis. For full thickness skin, mechanical cross sections of skin were made and optical sections were recorded parallel to the plane of cut. Phospholipid penetrated and was distributed fairly homogeneously in the lower dermis layers within 30 min of application regardless of liposome composition and the presence of Heparin. This rather quick penetration process seemed to follow distinct pathways along the epidermis and the upper dermis, notably the hair follicle route. Thus, a strong and in some respects composition-dependent interaction of phospholipids with skin is evident. These observations, however, are limited to the level of phospholipid molecules, rather than of entire liposomes interacting with skin.
authors.affiliation: Pharmaceutical Technology, Department of Pharmacy, University of Basel, Klingelbergstrasse 50, 4056, Basel, Switzerland.
authors.forename: G
authors.initials: G
authors.lastname: Betz
authors.forename: R
authors.initials: R
authors.lastname: Imboden
authors.forename: G
authors.initials: G
authors.lastname: Imanidis
mesh_terms: D000287:Administration, Topical; D000368:Aged; D000925:Anticoagulants / Q000008:administration & dosage / Q000493:pharmacokinetics; D004337:Drug Carriers; D005260:Female; D005456:Fluorescent Dyes; D006493:Heparin / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D066298:In Vitro Techniques; D008081:Liposomes / Q000737:chemistry*; D018613:Microscopy, Confocal; D008867:Microtomy; D008970:Molecular Weight; D012867:Skin / Q000737:chemistry*; D012869:Skin Absorption; D013109:Sphingomyelins / Q000737:chemistry*; D016707:Tissue Fixation
chemical_list: D000925:Anticoagulants; D004337:Drug Carriers; D005456:Fluorescent Dyes; D008081:Liposomes; D013109:Sphingomyelins; D006493:Heparin