title: Investigation of the Efficacy of Transdermal Penetration Enhancers Through the Use of Human Skin and a Skin Mimic Artificial Membrane.
abstract: The aim of this study was to investigate the behavior of promising penetration enhancers through the use of 2 different skin test systems. Hydrogel-based transdermal formulations were developed with ibuprofen as a nonsteroidal anti-inflammatory drug. Transcutol and sucrose esters were used as biocompatible penetration enhancers. The permeability measurements were performed with ex vivo Franz diffusion cell methods and a newly developed Skin Parallel Artificial Membrane Permeability Assays (PAMPA) model. Franz diffusion measurement is commonly used as a research tool in studies of diffusion through synthetic membranes in vitro or penetration through ex vivo human skin, whereas Skin PAMPA involves recently published artificial membrane-based technology for the fast prediction of skin penetration. It is a 96-well plate-based model with optimized artificial membrane structure containing free fatty acid, cholesterol, and synthetic ceramide analog compounds to mimic the stratum corneum barrier function. Transdermal preparations containing 2.64% of different sucrose esters and/or Transcutol and a constant (5%) of ibuprofen were investigated to determine the effects of these penetration enhancers. The study demonstrated the good correlation of the permeability data obtained through use of human skin membrane and the in vitro Skin PAMPA system. The Skin PAMPA artificial membrane serves as quick and relatively deep tool in the early stages of transdermal delivery systems, through which the enhancing efficacy of excipients can be screened so as to facilitate the choice of effective penetration components.
authors.affiliation: Department of Pharmaceutical Technology, University of Szeged, Szeged H-6720, Hungary; Gedeon Richter Plc., Budapest H-1103, Hungary.
authors.forename: Boglárka
authors.initials: B
authors.lastname: Balázs
authors.affiliation: Department of Pharmaceutical Chemistry, Semmelweis University, Budapest H-1092, Hungary.
authors.forename: Gábor
authors.initials: G
authors.lastname: Vizserálek
authors.affiliation: Department of Pharmaceutical Technology, University of Szeged, Szeged H-6720, Hungary.
authors.forename: Szilvia
authors.initials: S
authors.lastname: Berkó
authors.affiliation: Department of Pharmaceutical Technology, University of Szeged, Szeged H-6720, Hungary.
authors.forename: Mária
authors.initials: M
authors.lastname: Budai-Szűcs
authors.affiliation: Department of Applied Informatics, University of Szeged, Szeged H-6720, Hungary.
authors.forename: András
authors.initials: A
authors.lastname: Kelemen
authors.affiliation: Department of Pharmaceutical Chemistry, Semmelweis University, Budapest H-1092, Hungary; SinkoLAB Scientific, Sopron H-9400, Hungary.
authors.forename: Bálint
authors.initials: B
authors.lastname: Sinkó
authors.affiliation: Department of Pharmaceutical Chemistry, Semmelweis University, Budapest H-1092, Hungary.
authors.forename: Krisztina
authors.initials: K
authors.lastname: Takács-Novák
authors.affiliation: Department of Pharmaceutical Technology, University of Szeged, Szeged H-6720, Hungary.
authors.forename: Piroska
authors.initials: P
authors.lastname: Szabó-Révész
authors.affiliation: Department of Pharmaceutical Technology, University of Szeged, Szeged H-6720, Hungary. Electronic address: csanyi@pharm.u-szeged.hu.
authors.forename: Erzsébet
authors.initials: E
authors.lastname: Csányi
mesh_terms: D000279:Administration, Cutaneous; D032701:Biomimetics / Q000379:methods; D002518:Ceramides / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004058:Diffusion; D016503:Drug Delivery Systems / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D006801:Humans; D007052:Ibuprofen / Q000737:chemistry; D008567:Membranes, Artificial; D010539:Permeability; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry*; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D017768:Skin, Artificial
chemical_list: D002518:Ceramides; D005079:Excipients; D008567:Membranes, Artificial; D004364:Pharmaceutical Preparations; D007052:Ibuprofen
keywords: hydrogels; in vitro models; permeability; permeation enhancers; skin; surfactants; transdermal; transdermal drug delivery