title: New applications of phospholipid vesicle-based permeation assay: permeation model mimicking skin barrier.
abstract: The phospholipid vesicle-based permeation assay (PVPA), based on a tight barrier composed of liposomes mimicking cells, is providing an opportunity to predict passive drug permeability through biological membranes. Although it was originally developed to mimic the intestinal epithelia, this study focuses on its potential as a simple and affordable skin model for transdermal permeation of drug candidates and evaluation of various drugs and formulations at an early development stage. The changes induced in lipid composition of the lipid-based barriers to better mimic the in vivo stratum corneum lipid composition required optimization of liposomal properties and manufacturing conditions applied in barrier formation. The preparation conditions could be modified to prepare lipid-based barriers of different degrees of leakiness, potentially representing different degree of intact and compromised skin. The different PVPA models developed in this study appeared to be able to distinguish between drugs with different degrees of lipophilicity and penetration potential. Moreover, the PVPA can be produced in controlled and reproducible manner with different degree of leakiness. The model could therefore be applied in both pharmaceutical and cosmeceuticals manufacturing and also has the potential to provide deeper insight on safety of nanodelivery systems administered onto the skin.
authors.affiliation: Drug Transport and Delivery Research Group, Department of Pharmacy, University of Tromsø, Tromsø N-9037, Norway.
authors.forename: André
authors.initials: A
authors.lastname: Engesland
authors.forename: Merete
authors.initials: M
authors.lastname: Skar
authors.forename: Terkel
authors.initials: T
authors.lastname: Hansen
authors.forename: Nataša
authors.initials: N
authors.lastname: Škalko-Basnet
authors.forename: Gøril Eide
authors.initials: GE
authors.lastname: Flaten
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002518:Ceramides / Q000737:chemistry / Q000378:metabolism; D002784:Cholesterol / Q000737:chemistry / Q000378:metabolism; D002788:Cholesterol Esters / Q000737:chemistry / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D004817:Epidermis / Q000737:chemistry / Q000378:metabolism*; D005230:Fatty Acids, Nonesterified / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D008081:Liposomes / Q000737:chemistry / Q000378:metabolism*; D010539:Permeability; D010599:Pharmacokinetics; D010743:Phospholipids / Q000737:chemistry / Q000378:metabolism*; D012869:Skin Absorption
chemical_list: D002518:Ceramides; D002788:Cholesterol Esters; D005230:Fatty Acids, Nonesterified; D008081:Liposomes; D010743:Phospholipids; D002784:Cholesterol; C007045:cholesteryl sulfate