DERMAL ABSORPTION MODELS IN TOXICOLOGY AND PHARMACOLOGY doc

TLFeBOOK DERMAL ABSORPTION MODELS IN TOXICOLOGY AND PHARMACOLOGY DERMAL ABSORPTION MODELS IN TOXICOLOGY AND PHARMACOLOGY Edited by Jim E. Riviere North Carolina State University Raleigh, North Carolina A CRC title, part of the Taylor & Francis imprint, a member of the Taylor & Francis Group, the academic division of T&F Informa plc. Boca Raton London New York Published in 2006 by CRC Press Taylor & Francis Group 6000 Broken Sound Parkway NW, Suite 300 Boca Raton, FL 33487-2742 © 2006 by Taylor & Francis Group, LLC CRC Press is an imprint of Taylor & Francis Group No claim to original U.S. Government works Printed in the United States of America on acid-free paper 10 987654321 International Standard Book Number-10: 0-415-70036-1 (Hardcover) International Standard Book Number-13: 978-0-415-70036-8 (Hardcover) Library of Congress Card Number 2005041842 This book contains information obtained from authentic and highly regarded sources. Reprinted material is quoted with permission, and sources are indicated. A wide variety of references are listed. Reasonable efforts have been made to publish reliable data and information, but the author and the publisher cannot assume responsibility for the validity of all materials or for the consequences of their use. No part of this book may be reprinted, reproduced, transmitted, or utilized in any form by any electronic, mechanical, or other means, now known or hereafter invented, including photocopying, microfilming, and recording, or in any information storage or retrieval system, without written permission from the publishers. For permission to photocopy or use material electronically from this work, please access www.copyright.com (http://www.copyright.com/) or contact the Copyright Clearance Center, Inc. (CCC) 222 Rosewood Drive, Danvers, MA 01923, 978-750-8400. CCC is a not-for-profit organization that provides licenses and registration for a variety of users. For organizations that have been granted a photocopy license by the CCC, a separate system of payment has been arranged. Trademark Notice: Product or corporate names may be trademarks or registered trademarks, and are used only for identification and explanation without intent to infringe. Library of Congress Cataloging-in-Publication Data Dermal absorption models in toxicology and pharmacology / edited by Jim E. Riviere. p. ; cm. Includes bibliographical references and index. ISBN 0-415-70036-1 (alk. paper) 1. Dermatotoxicology Mathematical models. 2. Dermatologic agents Toxicology. 3. Health risk assessment. 4. Skin absorption. I. Riviere, J. Edmond (Jim Edmond) [DNLM: 1. Skin Absorption. 2. Models, Theoretical. 3. Risk Assessment. 4. Toxicology methods. WR 102 D4345 2005] RL803.D445 2005 616.5 dc22 2005041842 Visit the Taylor & Francis Web site at http://www.taylorandfrancis.com and the CRC Press Web site at http://www.crcpress.com Taylor & Francis Group is the Academic Division of T&F Informa plc. TF1776_Discl.fm Page 1 Friday, July 22, 2005 6:54 AM Preface Paradoxically, skin is both a primary barrier to systemic absorption of topically exposed chemicals and a portal to systemic delivery of transdermal medicaments. Knowledge of the factors that determine both extent and rate of chemical flux across the skin is an important component of both toxicology and pharmacology studies. The aim of this book is to provide current approaches and techniques by which dermal absorption may be quantitated utilizing end points relative to these two disciplines. There are a number of different experimental methods and mathematical modeling approaches in use today. Most are rooted in disciplines outside toxicology, yet their methods are applied to dermal absorption. This book serves as a bridge between general considerations in risk assessment and systemic toxicology texts. The first four chapters introduce and overview both the structure and function of skin as well as the in vitro and in vivo experimental approaches available for assessing dermal absorption of drugs and chemicals. This is followed by mathemat- ical or so-called in silico models to quantitating percutaneous absorption, including physiological-based pharmacokinetic modeling and quantitative structure–activity relationship methods. The next chapters deal with applications of these techniques to the risk assessment process. The remainder of the book discusses scenarios in which unique properties of the chemicals studied or the matrix in which they are exposed must be considered, including volatile compounds or dosing in soils. In many dermal absorption studies, unique properties of compounds or additives may alter a compound’s absorption. These include vasoactive chemicals, the use of penetration enhancers, or exposure in complex chemical mixtures. The book wraps up with a comparative analysis of chemical permeability in human and animal skin. This book reviews basic principles, presents in-depth discussions of the most widely used techniques, and offers select case studies of how these techniques have been applied under different scenarios. It serves as a concise introduction and review of the application of dermal absorption to problems in toxicology and pharmacology for both researchers in this field and graduate courses overviewing this area. Jim E. Riviere Editor Jim E. Riviere, D.V.M., Ph.D., is the Burroughs Wellcome Fund Distinguished Professor of Pharmacology, and the director of the Center for Chemical Toxicology Research and Pharmacokinetics at North Carolina State University (NCSU) in Raleigh, North Carolina. He received his B.S. (summa cum laude) and M.S. degrees from Boston College and his D.V.M. and Ph.D. in pharmacology from Purdue University and is a fellow of the Academy of Toxicological Sciences. He is a member of Phi Beta Kappa, Phi Zeta, and Sigma Xi. Dr. Riviere is an elected member of the Institute of Medicine of the National Academies and serves on the Science Board of the U.S. Food and Drug Administration. His honors include the 1999 O. Max Gardner Award from the Board of Governors of the Consolidated University of North Carolina, the 1991 Ebert Prize from the American Pharmaceutical Association, and the Harvey W. Wiley Medal and FDA Commissioner’s Special Citation. He is the editor of the Journal of Veterinary Pharmacology and Therapeutics and cofounder and codirector of the USDA Food Animal Residue Avoidance Databank (FARAD) program. He is past president of the Dermatotoxicology Specialty Section of the Society of Toxicology and is a member of the editorial board of Toxicology and Applied Pharmacology as well as Skin Pharmacology and Physiology . Dr. Riviere has had substantial extramural research support from both the government and the industry, totaling over $15 million in grants for which he was the principal investi- gator. He has published more than 380 full-length research papers and chapters. He holds five U.S. patents. Dr. Riviere has authored and edited 10 books on pharmaco- kinetics, toxicology, and food safety. His current research interests relate to risk assessment of chemical mixtures, absorption of drugs and chemicals across skin, and the food safety and pharmacokinetics of tissue residues in food-producing animals. Contributors Ronald E. Baynes Department of Population Health and Pathobiology Center for Chemical Toxicology Research and Pharmacokinetics College of Veterinary Medicine North Carolina State University Raleigh, North Carolina Keith R. Brain Welsh School of Pharmacy Cardiff University Cardiff, United Kingdom Robert L. Bronaugh Office of Cosmetics and Colors U.S. Food and Drug Administration Laurel, Maryland Annette L. Bunge Chemical Engineering Department Colorado School of Mines Golden, Colorado Rory Conolly National Center for Computational Toxicology U.S. Environmental Protection Agency Research Triangle Park, North Carolina Mark T.D. Cronin School of Pharmacy and Chemistry Liverpool John Moores University Liverpool, England Sheree E. Cross Therapeutics Research Unit School of Medicine Princess Alexandra Hospital University of Queensland Brisbane, Australia Richard H. Guy Departments of Biopharmaceutical Sciences and Pharmaceutical Chemistry University of California San Francisco, California and Department of Pharmacy and Pharmacology University of Bath United Kingdom Gerald B. Kasting College of Pharmacy The University of Cincinnati Medical Center Cincinnati, Ohio Jean-Paul Marty Laboratoire de Dermopharmacologie Université de Paris-Sud Châtenay-Malabry, France James N. McDougal Department of Pharmacology and Toxicology Wright State University School of Medicine Dayton, Ohio Babu M. Medi Department of Pharmaceutical Sciences College of Pharmacy North Dakota State University Fargo, North Dakota Nancy A. Monteiro-Riviere Department of Clinical Sciences Center for Chemical Toxicology Research and Pharmacokinetics College of Veterinary Medicine North Carolina State University Raleigh, North Carolina [...]... body, age, disease states, and other modulating factors, cell turnover and selfreplacement in normal human skin are thought to take approximately 1 month The mitotic rate increases after mechanical (tape stripping, incisions) or chemically induced injuries 6 DERMAL ABSORPTION MODELS IN TOXICOLOGY AND PHARMACOLOGY SC HF D HF SG A Figure 1.3 Light micrograph of pig skin depicting the stratum corneum (SC),... Sebaceous glands are usually found all over the body and are associated with hair follicles Their density can vary between anatomical site and between individuals (Figure 1.1, Figure 1.3) They are evaginations of the epithelial lining, 16 DERMAL ABSORPTION MODELS IN TOXICOLOGY AND PHARMACOLOGY and histologically are simple, branched, or compound alveolar glands containing a mass of epidermal cells... Estimating the Absorption of Volatile Compounds Applied to Skin 177 Gerald B Kasting Chapter 11 Modeling Dermal Absorption from Soils and Powders Using Stratum Corneum Tape-Stripping In Vivo 191 Annette L Bunge, Gilles D Touraille, Jean-Paul Marty, and Richard H Guy Chapter 12 Assessing Efficacy of Penetration Enhancers .213 Babu M Medi, Somnath Singh, and Jagdish Singh Chapter 13 Dermal. .. to the dermal root sheath of the hair follicle and extends toward the epidermis, where it connects to the papillary layer of the dermis On contraction, this muscle not only erects the hairs but also plays a role in emptying the sebaceous glands Glands of the Skin The excretory portion in the skin involves secretion from the sebaceous glands and the apocrine and eccrine sweat glands Sebaceous Glands Sebaceous... role in metabolizing keratin, collagen, melanin, lipid, carbohydrate, and vitamin D as well as in respiration and in biotransformation of xenobiotics Skin has many requirements to fulfill and is therefore a heterogeneous structure that contains many different cell types that will be discussed in detail RELEVANT ANATOMY AND PHYSIOLOGY Anatomically, skin is comprised of two principal and distinct components:... major role during early adolescence in acne vulgaris and in the evaluation of antiacne drug candidates It is thought that elderly people suffer from dry skin caused by low sebum secretion Sweat Glands — Sweat glands based on their morphologic and functional characteristics can be classified into apocrine or eccrine (merocrine) In domestic animals, the apocrine gland is extensively developed and found throughout... (1990) Interspecies and interregional analysis of the comparative histologic thickness and laser Doppler blood flow measurements at five cutaneous sites in nine species, J Invest Dermatol., 95:582–586 Monteiro-Riviere, N.A and Inman, A.O (1995) Indirect immunohistochemistry and immunoelectron microscopy distribution of eight epidermal -dermal junction epitopes in the pig and in isolated perfused skin treated... precursor protein involucrin and the putative precursor protein cornifin-α/SPRR1 The final product of this epidermal differentiation and keratinization process can be thought of as a stratum corneum envelope consisting of interlinked protein-rich cells containing a network of keratin filaments surrounded by a thicker plasma membrane coated by multilamellar lipid sheets This forms the typical “brick -and- mortar”... projections into the dermis The basement membrane has several functions: It maintains epidermal dermal adhesion, acts as a selective barrier between the epidermis and dermis by restricting some molecules and permitting the passage of others, in uences cell behavior and wound healing, and serves as a target for both immunologic (bullous diseases) and nonimmunologic injury (friction- or chemically induced... axis by having Langerhans cells process antigens and as an effector axis by setting up an in ammatory response to a foreign insult It has a well-developed stroma, which supports all other organs The skin has neurosensory properties by which receptors sense the modalities of touch, pain, and heat In addition, the skin functions as an endocrine organ by synthesizing vitamin D and is a target for androgens . TLFeBOOK DERMAL ABSORPTION MODELS IN TOXICOLOGY AND PHARMACOLOGY DERMAL ABSORPTION MODELS IN TOXICOLOGY AND PHARMACOLOGY Edited by Jim E. Riviere North Carolina. concise introduction and review of the application of dermal absorption to problems in toxicology and pharmacology for both researchers in this field and graduate