Dermatokinetics of Therapeutic Agents

211 Pages·2011·3.81 MB·English

by  S. Narasimha Murthy

Dermatokinetics of
Therapeutic Agents
Dermatokinetics of
Therapeutic Agents
Edited by
S. Narasimha Murthy
Boca Raton London New York
CRC Press is an imprint of the
Taylor & Francis Group, an informa business
CRC Press
Taylor & Francis Group
6000 Broken Sound Parkway NW, Suite 300
Boca Raton, FL 33487-2742
© 2011 by Taylor and Francis Group, LLC
CRC Press is an imprint of Taylor & Francis Group, an Informa business
No claim to original U.S. Government works
Printed in the United States of America on acid-free paper
10 9 8 7 6 5 4 3 2 1
International Standard Book Number-13: 978-1-4398-0478-0 (Ebook-PDF)
This book contains information obtained from authentic and highly regarded sources. Reasonable
efforts have been made to publish reliable data and information, but the author and publisher cannot
assume responsibility for the validity of all materials or the consequences of their use. The authors and
publishers have attempted to trace the copyright holders of all material reproduced in this publication
and apologize to copyright holders if permission to publish in this form has not been obtained. If any
copyright material has not been acknowledged please write and let us know so we may rectify in any
future reprint.
Except as permitted under U.S. Copyright Law, 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 stor-
age or retrieval system, without written permission from the publishers.
For permission to photocopy or use material electronically from this wor k, please access www.copy-
right.com (http://www.copyright.com/) or contact the Copyright Clearan ce Center, Inc. (CCC), 222
Rosewood Drive, Danvers, MA 01923, 978-750-8400. CCC is a not-for-profit organization that pro-
vides licenses and registration for a variety of users. For organizations that have been granted a pho-
tocopy 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.
Visit the Taylor & Francis Web site at
http://www.taylorandfrancis.com
and the CRC Press Web site at
http://www.crcpress.com
Dedicated to My Parents
Contents
Contributor Bios ........................................................................................................ix
Chapter 1 Introduction to Dermatokinetics ..........................................................1
Ya-Ting Wu, Yuri G. Anissimov, and Michael S. Roberts
Chapter 2 Theoretical Models for Dermatokinetics of Therapeutic Agents .......25
Rong Shi and Hartmut Derendorf
Chapter 3 Formulation Approaches to Modulate the Dermatokinetics
of Drugs ..............................................................................................67
Srinivasa Murthy Sammeta, Michael A Repka,
and S. Narasimha Murthy
Chapter 4 Conventional Methods of Cutaneous Drug Sampling .......................81
José Juan Escobar-Chávez, Miriam López-Cervantes,
and Adriana Ganem Rondero
Chapter 5 Cutaneous Microdialysis ..................................................................131
Grazia Stagni
Chapter 6 Sampling Substrates by Skin Permeabilization ...............................149
M. Begoña Delgado-Charro
Chapter 7 Spectroscopic Techniques in Dermatokinetic Studies .....................175
Georgios N. Stamatas
Chapter 8 Regulatory Perspective of Dermatokinetic Studies .........................193
April C. Braddy and Dale P. Conner
Index ......................................................................................................................203
vii
Contributor Bios
Yuri G. Anissimov, MSc (physics), PhD (applied mathematics), is a senior lec-
turer of mathematics at the School of Biomolecular and Physical Sciences, Griffith
University, Australia. His main research area is mathematical modeling of drug
transport through skin and liver kinetics.
April C. Braddy, PhD, is currently a team leader in the Division of Bioequivalence
in the Office of Generic Drugs, Center for Drug Evaluation and Research, U.S. FDA.
She joined the Division of Bioequivalence as a reviewer in 2006 and has been serv-
ing as a team leader since 2008. Dr. Braddy received her BSc in microbiology from
Clemson University in 2000 and her PhD in pharmacy (pharmaceutical sciences)
from the University of Florida, in 2004. She has been involved in several working
groups, which have been tasked with the review of bioequivalence regulatory sub-
missions for several therapeutic drug classes that include dermatologics. She has also
been involved in several research projects with a focus on pharmacodynamic model-
ing using WinNonlin and NONMEM software. Dr. Braddy has coauthored several
peer-reviewed research articles and book chapters, and has also served as a reviewer
for several journals in the field of medicinal chemistry.
Dale P. Conner, PharmD, is currently the director of the Division of Bioequivalence
1 Office of Generic Drugs, FDA, Rockville, Maryland. Dr. Conner received his BSc
in pharmacy from the Massachusetts College of Pharmacy in 1979 and his PharmD
from the University of Florida, in 1983. From 1983 to 1985, he completed a postdoc-
toral fellowship in clinical pharmacology in the Division of Clinical Pharmacology
of Thomas Jefferson University, Pennsylvania. He then joined the faculty of the
Uniformed Services University of the Health Sciences as an assistant, and later asso-
ciate, professor in the Division of Clinical Pharmacology. From 1992 to 1994, he was
the director of pharmacokinetics for Scios Nova, Inc. From 1995 to 1997, he held the
position at FDA of team leader for clinical pharmacology and biopharmaceutics in
the areas of pulmonary, allergy, drug abuse, anesthesia, and critical care drug prod-
ucts. Dr. Conner is board certified in applied pharmacology by the American Board
of Clinical Pharmacology. His research interests have included pharmacokinetics,
drug metabolism, analytical methods, transcutaneous measurement of drugs, mea-
surement of drug effects on the skin, development of nasal and inhalation products,
and drug therapy of sepsis and ARDS.
M. Begoña Delgado-Charro, PhD, qualified as a pharmacist and received her PhD
from the University of Santiago de Compostela (1990). She was an MEC-Fulbright
fellow at University of California, San Francisco (1991–1993), where she specialized in
iontophoresis. She worked at the Universities of Santiago de Compostela and Geneva
and moved to the University of Bath, United Kingdom, in 2004, where she currently
works as a senior lecturer. Her teaching activity concerns pharmaceutics, drug delivery,
ix
x Contributor Bios
and pharmacokinetics. Her research involves the use of iontophoresis to optimize
transdermal drug delivery, drug delivery to the nail and as a tool for noninvasive drug
monitoring and pharmacokinetics. Her work has been funded by the Swiss National
Science Foundation, Parkinson’s Disease Society, United Kingdom, MRC, NHS-NIC,
and by several pharmaceutical companies. Dr. Delgado-Charro is a member of the
IATDMCT, EUFEPS, APV, APS, CRS and the Medicines for Children Research
Network. She has published 68 peer-reviewed articles in the scientific literature, 9 book
chapters, 100 congress abstracts, and has several patents in the field of iontophoresis.
Hartmut Derendorf, PhD, is a distinguished professor and chairman of the
Department of Pharmaceutics at the University of Florida College of Pharmacy.
Professor Derendorf has published over 340 scientific publications and 6 text-
books in English and German. He is an associate editor of the Journal of Clinical
Pharmacology, the European Journal of Pharmaceutical Sciences, and the editor
of the International Journal of Clinical Pharmacology and Therapeutics and Die
Pharmazie. Professor Derendorf has served as president of the American College
of Clinical Pharmacology (ACCP) and president of the International Society of
Anti-Infective Pharmacology (ISAP). He was awarded the Distinguished Research
Award and the Nathaniel T. Kwit Distinguished Service Award of ACCP, the
Research Achievement Award in Clinical Science of the American Association
of Pharmaceutical Sciences (AAPS), and the Volwiler Award of the American
Association of Colleges of Pharmacy (AACP).
José Juan Escobar-Chávez, PhD, is a professor at the Faculty of Chemistry and
Pharmacy, University of Mexico (UNAM). His research interests are in the topical
and transdermal delivery of drugs and include the use of tape-stripping technique
to quantify the amount of drug in layers of stratum corneum, the use of TEWL and
ATR/FTIR to show the changes of skin as a result of the use of chemical enhanc-
ers, the use of iontophoresis and microneedles in the transdermal administration of
drugs, and the development and characterization of transdermal patches and gels.
The application of nanotechnology in drug delivery is another major research inter-
est. He has published a number of research papers in these areas. He has written
three book chapters and edited an e-book with Bentham Science Publishers.
Miriam López-Cervantes, PhD, is a professor at the Faculty of Chemistry and
Pharmacy, University of Mexico, and qualifier at Comisión Federal de Prevención
contra Riesgos Sanitarios (COFEPRIS). Dr. López-Cervantes’s research interests are
in the topical and transdermal delivery of drugs and include the use of the chemical
and physical enhancers for the absorption of substances through the skin, like lau-
rocapram and its derivatives, and development and characterization of transdermal
patches and gels.
S. Narasimha Murthy, PhD, is an assistant professor of pharmaceutics at the
University of Mississippi. He received his PhD in pharmaceutics from Bangalore
University, India, in 2003. He completed his postdoctoral research at Roswell Park
Cancer Institute, New York, in 2005. His research interests are mainly in the area
Contributor Bios xi
transdermal and trans-ungual drug delivery. Dr. Murthy has developed several inno-
vative technologies to enhance drug delivery across the skin and nail plate. He has
published over 60 research papers in peer-reviewed scientific journals. He is the edi-
tor of the book Dermatokinetics of Therapeutic Agents.
Michael A. Repka, PhD, is chair and associate professor of the Department of
Pharmaceutics at the University of Mississippi, as well as director, Center for Thermal
Pharmaceutical Processing. He joined the faculty at University of Mississippi after
receiving his PhD from the University of Texas College of Pharmacy. His research
interests include oral transmucosal and transdermal/trans-nail delivery systems.
Many of these systems are directed toward the solubilization and delivery of poorly
soluble bioactives via hot-melt extrusion technology, which is a primary focus of his
research. Polymeric drug delivery design, stabilization of conventional and novel
drug delivery systems, formulation and process development for natural products
such as tetrahydrocannabinol and pro-drugs, in addition to antifungal/antibacterial
agents and vaccines, are also a significant part of his research. Dr. Repka’s publica-
tions include over 60 peer-reviewed journal articles and well over 200 presentations
at national/international scientific meetings.
Michael Roberts, B Pharm, MSc, PhD, DSc, MBA, FACP, is an Australian National
Health and Medical Research senior principal research fellow, professor of therapeu-
tics and pharmaceutical science at the University of South Australia (UniSA), and a
professor of clinical pharmacology and therapeutics in the School of Medicine at the
University of Queensland (UQ). He is director of the Therapeutics Research Centre
with the UniSA Unit based at the Queen Elizabeth Hospital in Adelaide and the UQ
Unit based at the Princess Alexandra Hospital (PAH) in Brisbane. He has more than
350 peer-reviewed research publications (more than 625 communications in total,
including 46 book chapters) and is the coeditor of three research books on topical
drug delivery as well as three others. Two of his main research interests are topical
drug delivery and pharmacokinetics.
Flora Adriana Ganem Rondero, PhD, obtained his PhD in pharmaceutical
sciences at the University of Geneva (Switzerland) and Claude Bernard–Lyon I
(France). Since 1988, Dr. Rondero has worked in pharmaceutical technology at
Universidad Nacional Autónoma de México. She was appointed in the current
position in the laboratory of pharmaceutical technology (Facultad de Estudios
Superiores Cuautitlán, Universidad Nacional Autónoma de México) in 1998. Her
research interests are in the area of permeation enhancers in topical and transder-
mal drug delivery.
Srinivasa Murthy Sammeta is a PhD student of Dr. S. Narasimha Murthy in the
Department of Pharmaceutics at the University of Mississippi. Sammeta has pub-
lished 15 research papers on topics related to transdermal and topical drug delivery
and sampling. He is an NIH pre-doctoral fellow, and a member of the American
Association of Pharmaceutical Scientists and Rho Chi. Sammeta received his mas-
ter’s degree in 2006 from Rajiv Gandhi University of Health Sciences in India.
xii Contributor Bios
Rong Shi received her master of science degree in chemistry from the University of
Missouri-Rolla (now Missouri University of Science and Technology). Since 2006,
she has been pursuing her doctoral research in pharmaceutics at the University of
Florida, under the supervision of Dr. Hartmut Derendorf.
Grazia Stagni, MS, PhD, is an associate professor of pharmaceutics at Long Island
University, Brooklyn, New York. She received her laurea in medicinal chemistry and
pharmaceutical technology from the Università degli Studi of Bologna in Italy and
her master’s and PhD in pharmaceutics from the University of Texas at Austin. After
graduation, she joined the Division of Clinical Pharmacology at the University of
Texas Health Science Research Center in San Antonio as a research fellow. In 2000,
Dr. Stagni joined the faculty at Long Island University. Her research interests include
pharmacokinetics and pharmacodynamics, microdialysis in skin, and dermal and
transdermal drug delivery.
Georgios N. Stamatas, PhD, graduated with honors from the Department of
Chemical Engineering at the Aristotle University of Thessaloniki, Greece. He
received his PhD in chemical/biomedical engineering from Rice University, Houston,
Texas. Following a postdoctoral fellowship in tissue engineering at Rice University,
Dr. Stamatas joined the R&D group of Johnson & Johnson Consumer Products at
Skillman, New Jersey, and later at Issy-les-Moulineaux, France. His research focuses
on biomedical applications in dermatology with an emphasis on skin biophysics for
the development of noninvasive in vivo methods. His current interests include skin
physiology and development of infant skin during the first years of life. Dr. Stamatas
has authored over 40 scientific publications, over 100 meeting abstracts, and 8 inter-
national patent applications.
Ya-Ting Wu is a PhD student at the University of Queensland, Australia. Her
research interests include topics related to drug delivery to the hair follicles and in
developing a novel treatment for common skin diseases such as hair loss, acne, and
rosacea.