New tools and approaches for predicting skin permeability.

This article reviews some new mathematical models and techniques used to predict and understand percutaneous penetration and transdermal delivery. These models are also useful for various enhancement strategies that can be used in dermal-penetration and formulation development studies. If appropriate, biophysical techniques can be combined with these new mathematical models and statistical analyses and it will be possible to understand the factors affecting penetration of molecules through skin. These factors, or parameters, can then be used to control the penetration rate when effective transdermal delivery or therapy is required or targeted.

[1]  K. A. Walters,et al.  Dermatological And Transdermal Formulations , 2002 .

[2]  J. Hadgraft,et al.  The effects of Azone and capsaicin on the permeation of naproxen through human skin. , 1999, International journal of pharmaceutics.

[3]  G. Flynn,et al.  Transdermal Delivery of Narcotic Analgesics: Comparative Permeabilities of Narcotic Analgesics Through Human Cadaver Skin , 1989, Pharmaceutical Research.

[4]  A. Eisen,et al.  Structure and organization of mammalian stratum corneum. , 1971, Journal of ultrastructure research.

[5]  H. Maibach,et al.  Topical Drug Bioavailability, Bioequivalence, and Penetration , 1993, Springer US.

[6]  M. H. Ross,et al.  Histology: A Text and Atlas , 1985 .

[7]  Yie W. Chien,et al.  Development of Transdermal Drug Delivery Systems , 1987 .

[8]  Michael S. Roberts,et al.  Epidermal permeability penetrant structure relationships .1. An analysis of methods of predicting penetration of monofunctional solutes from aqueous solutions , 1995 .

[9]  J Hadgraft,et al.  Epidermal permeability-penetrant structure relationships: 4, QSAR of permeant diffusion across human stratum corneum in terms of molecular weight, H-bonding and electronic charge. , 2000, International journal of pharmaceutics.

[10]  P. Elias,et al.  Percutaneous transport in relation to stratum corneum structure and lipid composition. , 1981, The Journal of investigative dermatology.

[11]  Y Martín-Biosca,et al.  Evaluation of the pH effect of formulations on the skin permeability of drugs by biopartitioning micellar chromatography. , 2004, Journal of chromatography. A.

[12]  R. Guy,et al.  Transdermal drug delivery : developmental issues and research initiatives , 1989 .

[13]  C. Ho.  Probabilistic modeling of percutaneous absorption for risk-based exposure assessments and transdermal drug delivery , 2004 .

[14]  Russell O. Potts,et al.  Macro- and molecular physical-chemical considerations in understanding drug transport in the stratum corneum , 1985 .

[15]  G. Flynn,et al.  Permeation of hairless mouse skin II: membrane sectioning techniques and influence on alkanol permeabilities. , 1981, Journal of pharmaceutical sciences.

[16]  Jonathan Hadgraft,et al.  Ab initio prediction of human skin permeability coefficients , 1994 .

[17]  Jonathan Hadgraft,et al.  Transdermal drug delivery: A perspective , 1987 .

[18]  Michael S. Roberts,et al.  Epidermal permeability — Penetrant structure relationships: 3. The effect of hydrogen bonding interactions and molecular size on diffusion across the stratum corneum , 1996 .

[19]  David R. Friend,et al.  In vitro skin permeation techniques , 1992 .

[20]  J. Lademann,et al.  Comparison of four different in vitro systems to study the reservoir capacity of the stratum corneum. , 2005, Journal of controlled release : official journal of the Controlled Release Society.

[21]  Fumiyoshi Yamashita,et al.  Prediction of human skin permeability using a combination of molecular orbital calculations and artificial neural network. , 2002, Biological & pharmaceutical bulletin.

[22]  Angela K. Pannier,et al.  Fuzzy Modeling of Skin Permeability Coefficients , 2004, Pharmaceutical Research.

[23]  M. Goosen,et al.  Transdermal delivery of peptide and protein drugs: An overview , 1995 .

[24]  G. Marshall.  Computer-aided drug design. , 1987, Annual review of pharmacology and toxicology.

[25]  M. Roberts,et al.  Permeability of human epidermis to phenolic compounds , 1977, The Journal of pharmacy and pharmacology.

[26]  M. Medina-Hernández,et al.  Biopartitioning micellar chromatography to predict skin permeability. , 2003, Biomedical chromatography : BMC.

[27]  Geoffrey Lee.  Prediction of Percutaneous Penetration , 1997 .

[28]  A. Michaels,et al.  Drug permeation through human skin: Theory and invitro experimental measurement , 1975 .

[29]  M. Turowski,et al.  Keratin immobilized on silica as a new stationary phase for chromatographic modelling of skin permeation. , 1997, Journal of pharmaceutical and biomedical analysis.

[30]  T E McKone,et al.  Estimating skin permeation. The validation of five mathematical skin permeation models. , 1995, Chemosphere.

[31]  L Landmann,et al.  Epidermal permeability barrier: transformation of lamellar granule-disks into intercellular sheets by a membrane-fusion process, a freeze-fracture study. , 1986, The Journal of investigative dermatology.

[32]  Samir Mitragotri,et al.  Modeling skin permeability to hydrophilic and hydrophobic solutes based on four permeation pathways. , 2003, Journal of controlled release : official journal of the Controlled Release Society.

[33]  Russell O. Potts,et al.  Predicting Skin Permeability , 1992, Pharmaceutical Research.

[34]  N el Tayar,et al.  Percutaneous penetration of drugs: a quantitative structure-permeability relationship study. , 1991, Journal of pharmaceutical sciences.

[35]  I. Tuncer Degim,et al.  Understanding Skin Penetration: Computer Aided Modeling and Data Interpretation , 2005 .

[36]  R. Scheuplein,et al.  Mechanism of percutaneous adsorption. I. Routes of penetration and the influence of solubility. , 1965, The Journal of investigative dermatology.

[37]  J. Hadgraft,et al.  Comparison of Franz cells and microdialysis for assessing salicylic acid penetration through human skin. , 2004, International journal of pharmaceutics.

[38]  M. Kawai,et al.  Importance of intercellular lipids in water-retention properties of the stratum corneum: induction and recovery study of surfactant dry skin , 2004, Archives of Dermatological Research.

[39]  R. Scheuplein,et al.  Permeability of the Skin , 1971 .

[40]  R. Daynes,et al.  Skin immunology: The Achilles heel to transdermal drug delivery☆ , 1987 .

[41]  K A Holbrook,et al.  Regional differences in the thickness (cell layers) of the human stratum corneum: an ultrastructural analysis. , 1974, The Journal of investigative dermatology.

[42]  A. Buciński,et al.  Hydrophobicity parameter from high-performance liquid chromatography on an immobilized artificial membrane column and its relationship to bioactivity , 1995 .

[43]  B. Berner.  Book reviewPrediction of percutaneous penetration. methods, measurements, and modelling: R.C. Scott, R.H. Guy and J. Hadgraft (Editors) IBC Technical Services Ltd., London, 1990, pp., £75.00 , 1990 .

[44]  Jyh-Shing Roger Jang,et al.  ANFIS: adaptive-network-based fuzzy inference system , 1993, IEEE Trans. Syst. Man Cybern..

[45]  G. L. Tong,et al.  Physicochemical Properties and Percutaneous Absorption of Drugs , 1973 .

[46]  M. Kerscher,et al.  Skin ceramides : Structure and function , 1991 .

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

[48]  Jonathan Hadgraft,et al.  Skin permeability data: Anomalous results , 1998 .

[49]  Samir Mitragotri,et al.  A theoretical analysis of permeation of small hydrophobic solutes across the stratum corneum based on Scaled Particle Theory. , 2002, Journal of pharmaceutical sciences.

[50]  Michael H. Abraham,et al.  The Factors that Influence Skin Penetration of Solutes * , 1995 .

[51]  M. Abraham,et al.  Algorithms for Skin Permeability Using Hydrogen Bond Descriptors: the Problem of Steroids * , 1997, The Journal of pharmacy and pharmacology.

[52]  P. Elias,et al.  The biochemistry and function of stratum corneum lipids. , 1991, Advances in lipid research.

[53]  Jonathan Hadgraft,et al.  Prediction of skin penetration using artificial neural network (ANN) modeling. , 2003, Journal of pharmaceutical sciences.

[54]  Peter Politzer,et al.  Quantitative treatments of solute/solvent interactions , 1994 .

[55]  J. Hadgraft,et al.  Epidermal lipids and topical drug delivery. , 1992, Seminars in dermatology.

[56]  B. Poulsen,et al.  Absorption of Drugs through the Skin , 1908, The Hospital.