Transdermal drug delivery in vitro using diffusion cells.

The assessment of percutaneous absorption of molecules is a very important step in the evaluation of any dermal or transdermal drug delivery system. In order to perform percutaneous drug absorption studies, it is essential that the methods are standardized and that the integrity of the skin is monitored and maintained to ensure that the data obtained are valid and relevant. Reproducible data on percutaneous absorption in humans are as well required to predict the systemic risk from dermal exposure to chemicals, such as hazardous substances at the workplace, agrochemicals and cosmetic ingredients. In vitro and animal models provide important tools for screening a series of drug formulations, evaluation of skin permeation enhancing properties and mechanism of action of the carrier systems and estimation of rank of skin transport for a series of drug molecules. In this review, we have summarized in vitro testing of skin absorption using static Franz-type diffusion cells.

[1]  Howard I. Maibach,et al.  Percutaneous Absorption: Drugs, Cosmetics, Mechanisms, Methods, Fourth Edition , 2005 .

[2]  Robert L. Bronaugh Methods for in Vitro Percutaneous Absorption , 1995 .

[3]  J Kao,et al.  Cutaneous metabolism of xenobiotics. , 1990, Drug metabolism reviews.

[4]  P. Blondeel,et al.  A new discriminative criterion for the development of Franz diffusion tests for transdermal pharmaceuticals. , 2010, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.

[5]  J. Bouwstra,et al.  Structure of the skin barrier and its modulation by vesicular formulations. , 2003, Progress in lipid research.

[6]  S. M. Harrison,et al.  Effects of freezing on human skin permeability , 1984, The Journal of pharmacy and pharmacology.

[7]  Biana Godin,et al.  Transdermal skin delivery: predictions for humans from in vivo, ex vivo and animal models. , 2007, Advanced drug delivery reviews.

[8]  G. P. Martin,et al.  Variability in human skin permeability in vitro: comparing penetrants with different physicochemical properties. , 2007, Journal of pharmaceutical sciences.

[9]  R. F. Fedors,et al.  A method for estimating both the solubility parameters and molar volumes of liquids , 1974 .

[10]  Hope Mj,et al.  Liposomes. A perspective for dermatologists. , 1993 .

[11]  J. Bos,et al.  The 500 Dalton rule for the skin penetration of chemical compounds and drugs , 2000, Experimental dermatology.

[12]  B. Kemppainen,et al.  Methods for Skin Absorption , 1990 .

[13]  B. Testa,et al.  The skin as a drug-metabolizing organ. , 1978, Drug metabolism reviews.

[14]  J. Heylings,et al.  Multi-species assessment of electrical resistance as a skin integrity marker for in vitro percutaneous absorption studies. , 2004, Toxicology in vitro : an international journal published in association with BIBRA.

[15]  A. Sakr,et al.  Maintenance of skin viability during in vitro percutaneous absorption/metabolism studies. , 1989, Toxicology and applied pharmacology.

[16]  B. Spiegeleer,et al.  Quality analytics of internet pharmaceuticals , 2010, Analytical and bioanalytical chemistry.

[17]  James N McDougal,et al.  Skin absorption and human risk assessment. , 2002, Chemico-biological interactions.

[18]  P Sartorelli,et al.  In vitro predictions of skin absorption of caffeine, testosterone, and benzoic acid: a multi-centre comparison study. , 2004, Regulatory toxicology and pharmacology : RTP.

[19]  R. Bronaugh,et al.  Methods for in vitro percutaneous absorption studies IV: The flow-through diffusion cell. , 1985, Journal of pharmaceutical sciences.

[20]  H. Maibach,et al.  Percutaneous Absorption: Mechanisms-Methodology-Drug Delivery , 1989 .

[21]  S. Hotchkiss,et al.  Evaluation of Barrier Creams against Sulphur Mustard , 2002, Skin Pharmacology and Physiology.

[22]  Geoffrey Lee,et al.  Drug Permeation through Human Skin: I. Effects of Storage Conditions of Skin , 1982 .

[23]  Eric Deconinck,et al.  Transdermal penetration behaviour of drugs: CART-clustering, QSPR and selection of model compounds. , 2007, Bioorganic & medicinal chemistry.

[24]  B. van Ravenzwaay,et al.  A comparison between in vitro rat and human and in vivo rat skin absorption studies , 2004, Human & experimental toxicology.

[25]  M. Bracher,et al.  Percutaneous absorption of hair dyes : an interlaboratory comparison of in vivo and in vitro data with rat and pig , 1994 .

[26]  J A Bouwstra,et al.  Skin structure and mode of action of vesicles. , 2002, Advanced drug delivery reviews.

[27]  R. Scott,et al.  Further validation of an in vitro method to reduce the need for in vivo studies for measuring the absorption of chemicals through rat skin. , 1992, Fundamental and applied toxicology : official journal of the Society of Toxicology.

[28]  D Guest,et al.  A comparative study of the rates of in vitro percutaneous absorption of eight chemicals using rat and human skin. , 1992, Fundamental and applied toxicology : official journal of the Society of Toxicology.

[29]  T. Franz Percutaneous absorption on the relevance of in vitro data. , 1975, The Journal of investigative dermatology.

[30]  Howard I. Maibach,et al.  Evaluation of the Barrier Function of Skin Using Transepidermal Water Loss (TEWL): A Critical Overview , 2014 .

[31]  J. Bouwstra,et al.  Water distribution and natural moisturizer factor content in human skin equivalents are regulated by environmental relative humidity. , 2008, The Journal of investigative dermatology.

[32]  J. J. van de Sandt,et al.  Comparative in vitro-in vivo percutaneous absorption of the pesticide propoxur. , 2000, Toxicological sciences : an official journal of the Society of Toxicology.

[33]  Majella E Lane,et al.  Skin penetration enhancers. , 2013, International journal of pharmaceutics.

[34]  R H Guy,et al.  Iontophoresis—Recent Developments * , 1998, The Journal of pharmacy and pharmacology.

[35]  K. Vávrová,et al.  Ammonium carbamates as highly active transdermal permeation enhancers with a dual mechanism of action. , 2011, Journal of controlled release : official journal of the Controlled Release Society.

[36]  T. Redelmeier,et al.  Skin Barrier: Principles of Percutaneous Absorption , 1996 .

[37]  A. Watkinson Dermal and Transdermal Drug Delivery , 2008 .

[38]  Michael S Roberts,et al.  Molecular size as the main determinant of solute maximum flux across the skin. , 2004, The Journal of investigative dermatology.

[39]  M. Schäfer-Korting,et al.  The Phenion® Full-Thickness Skin Model for Percutaneous Absorption Testing , 2009, Skin Pharmacology and Physiology.

[40]  C. Hansen,et al.  Permeability of commercial solvents through living human skin. , 1995, American Industrial Hygiene Association journal.

[41]  Absorption Enhancers: Applications and Advances , 2012, The AAPS Journal.

[42]  J. Weaver,et al.  Comparison of the effects of short, high-voltage and long, medium-voltage pulses on skin electrical and transport properties. , 1999, Journal of controlled release : official journal of the Controlled Release Society.

[43]  J. Zbytovská,et al.  Amphiphilic transdermal permeation enhancers: structure-activity relationships. , 2005, Current medicinal chemistry.

[44]  Mark T D Cronin,et al.  Quantitative structure-activity relationships (QSARs) for the prediction of skin permeation of exogenous chemicals. , 2002, Chemosphere.

[45]  K. Sugibayashi,et al.  Species differences in percutaneous absorption of nicorandil. , 1991, Journal of pharmaceutical sciences.

[46]  R. Zendzian Dermal absorption of pesticides in the rat. , 2000, AIHAJ : a journal for the science of occupational and environmental health and safety.

[47]  Robert Langer,et al.  Transdermal drug delivery , 2008, Nature Biotechnology.

[48]  G. S. Hawkins,et al.  Development of an in vitro model for determining the fate of chemicals applied to skin. , 1984, Fundamental and applied toxicology : official journal of the Society of Toxicology.

[49]  H. Maibach,et al.  Effects of Skin Occlusion on Percutaneous Absorption: An Overview , 2001, Skin Pharmacology and Physiology.

[50]  Ian Colbeck,et al.  Human Exposure to Pollutants via Dermal Absorption and Inhalation , 2010 .