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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5636_Библиотеки_им_академика_М_И_Перельмана
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AAPS Advances in the Pharmaceutical Sciences Series
For other titles published in this series, go to
http://www.springer.com/series/8825
Uday B. Kompella • Henry F. Edelhauser
Editors
Drug Product Development
for the Back of the Eye
Editors
https://t.me/med1917
Uday B. Kompella
Pharmaceutical Sciences & Ophthalmology
Nanomedicine and Drug Delivery
Laboratory
University of Colorado
Aurora, CO, USA
Uday.Kompella@ucdenver.edu
Henry F. Edelhauser
Department of Ophthalmology
Emory University Eye Center
Emory University
Atlanta, GA, USA
ophthfe@emory.edu
ISSN 2210-7371 e-ISSN 2210-738X
ISBN 978-1-4419-9919-1 e-ISBN 978-1-4419-9920-7
DOI 10.1007/978-1-4419-9920-7
Springer New York Dordrecht Heidelberg London
Library of Congress Control Number: 2011931861
© American Association of Pharmaceutical Scientists, 2011
All rights reserved. This work may not be translated or copied in whole or in part without the written
permission of the publisher (Springer Science+Business Media, LLC, 233 Spring Street, New York,
NY 10013, USA), except for brief excerpts in connection with reviews or scholarly analysis. Use in
connection with any form of information storage and retrieval, electronic adaptation, computer software,
or by similar or dissimilar methodology now known or hereafter developed is forbidden.
The use in this publication of trade names, trademarks, service marks, and similar terms, even if they are
not identified as such, is not to be taken as an expression of opinion as to whether or not they are subject
to proprietary rights.
While the advice and information in this book are believed to be true and accurate at the date of going to
press, neither the authors nor the editors nor the publisher can accept any legal responsibility for any
errors or omissions that may be made. The publisher makes no warranty, express or implied, with respect
to the material contained herein.
Printed on acid-free paper
Springer is part of Springer Science+Business Media (www.springer.com)
Preface
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Age-related macular degeneration and macular edema are major vision-threatening
disorders of the back of the eye. The first therapeutic agents for treating these diseases, Macugen™ (Pfizer, a nucleic acid-based drug), Lucentis™ (Genentech; a
protein drug), and Ozurdex™ (Allergan; a small molecule drug in a biodegradable,
injectable implant) were approved by the US FDA in 2004, 2006, and 2009, respectively.
Lucentis is already a billion-dollar product. With the success of Lucentis, there is an
escalated activity for drug development for the back of the eye. Also, as evident
earlier, a variety of therapeutic agents including nucleic acids, protein drugs, and
small molecules are making inroads into the emerging back of the eye drug product
market. Further, some unique delivery systems including surgically placed and
injectable non-degradable implants have pioneered zero-order release of small molecule drugs for treating back of the eye diseases. Vitrasert™ and Retisert™, surgically placed intravitreal implants, were approved in 1996 and 2005, respectively, for
treating cytomegalovirus retinitis and chronic non-infectious uveitis. Iluvien™, an
injectable, third-generation non-degradable implant for the eye, is in late stage clinical trials for treating diabetic macular edema. In addition, cell encapsulating implants
for long-term delivery of growth factors are undergoing late-phase clinical trials for
treating age-related macular degeneration. It is anticipated that drug development
for the back of the eye will take a center stage in ophthalmic drug product development during the next decade. Currently available textbooks do not address drug
delivery and product development challenges and the selection of delivery systems
for various classes of therapeutic agents in a systematic manner. To cater to this
unmet need, we undertook the task of preparing a comprehensive textbook in the
area of drug product development for the back of the eye, authored by ocular drug
delivery experts, representing academic, clinical, and industrial organizations.
After discovering a drug molecule with therapeutic activity in the back of the eye
tissues, a drug delivery scientist is presented with a multitude of options for routes
of drug delivery and choice of delivery system. Chapter 1 presents a rational
approach for selecting routes of administration and delivery systems for the back of
the eye. Routine ocular pharmacokinetic studies are not yet viable in humans for
the purpose of back of the eye drug product development, necessitating the use of
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preclinical models for such studies. Since eye tissue sampling cannot be performed
continuously, several animals are sacrificed for a single pharmacokinetic study.
Microdialysis of ocular fluids and fluorophotometry, two alternatives that provide
full pharmacokinetic profile with limited number of animals, are presented in
Chapters 2 and 3, respectively.
Chapters 4–8 discuss systemic, topical, intravitreal, transscleral, intrascleral, and
suprachoroidal routes of drug administration and the underlying barriers and drug
delivery principles in treating back of the eye diseases. Integral for any drug product
development for the back of the eye are drug delivery systems. Chapters 9–16 discuss a variety of drug delivery systems, devices, and physical methods intended for
drug delivery to the back of the eye. The delivery systems discussed include nanoparticles, microparticles, hydrogels, implants, and refillable devices. In addition,
these chapters discuss physical approaches of drug delivery including ultrasmall
microneedles for minimally invasive delivery and iontophoresis and electrophoresis
for noninvasive drug and gene delivery. Further, as discussed in Chapters 17 and 18,
even simple dosage forms such as drug solutions of macromolecules (e.g., Lucentis
and Macugen) and drug suspensions of small molecules (e.g., Trivaris™ and
Triescence™) are viable for prolonged back of the eye drug delivery.
No drug product enters the US market without receiving approval from the FDA.
The FDA provides guidelines that are useful in ensuring the safety and efficacy of
drug products. Chapter 19 describes these considerations. Key to assessing drug
efficacy in the clinical setting is the identification and assessment of appropriate
endpoints and biomarkers, as described in Chapter 19. Ongoing drug product development depends on the discovery of new diseases, targets and drug molecules.
Chapters 21 and 22 present druggable targets and several therapeutic agents for
treating back of the eye diseases.
This volume is intended for ophthalmic researchers, drug formulation scientists,
drug delivery scientists, drug disposition scientists, and clinicians involved in
designing and developing novel therapeutics for the back of the eye diseases.
Further, this book will serve as a textbook for students in various disciplines including ophthalmology, pharmaceutical sciences, drug delivery, and biomedical
engineering.
We are very thankful to Ms. Kristen Grompone for assisting us with the book
preparation by communicating with the authors, coordinating manuscript submissions, and formatting the various chapters for publication. Drug Product Development
for the Back of the Eye would not have been possible without the support of several
authors, colleagues, and students in training. We are indebted to all those who made
this volume possible.
Aurora, CO
Atlanta, GA Henry F. Edelhauser
Uday B. Kompella
Contents
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1 Selection of Drug Delivery Approaches for the Back of the Eye:
Opportunities and Unmet Needs ........................................................... 1
David A. Marsh
2 Microdialysis for Vitreal Pharmacokinetics ......................................... 21
Ravi D. Vaishya, Hari Krishna Ananthula, and Ashim K. Mitra
3 Fluorophotometry for Pharmacokinetic Assessment .......................... 47
Bernard E. McCarey
4 Systemic Route for Retinal Drug Delivery:
Role of the Blood-Retinal Barrier ......................................................... 85
Masanori Tachikawa, Vadivel Ganapathy, and Ken-ichi Hosoya
5 Topical Drug Delivery to the Back of the Eye ...................................... 111
Thomas Gadek and Dennis Lee
6 Principles of Retinal Drug Delivery from Within the Vitreous .......... 125
Clive G. Wilson, Lay Ean Tan, and Jenifer Mains
7 Transscleral Drug Delivery .................................................................... 159
Dayle H. Geroski and Henry F. Edelhauser
8 Suprachoroidal and Intrascleral Drug Delivery .................................. 173
Timothy W. Olsen and Brian C. Gilger
9 Advances in Biodegradable Ocular Drug Delivery Systems ............... 185
Susan S. Lee, Patrick Hughes, Aron D. Ross,
and Michael R. Robinson
10 Microparticles as Drug Delivery Systems
for the Back of the Eye ........................................................................... 231
Rocío Herrero-Vanrell
11 Nanotechnology and Nanoparticles ....................................................... 261
Shelley A. Durazo and Uday B. Kompella
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12 Hydrogels for Ocular Posterior Segment Drug Delivery .................... 291
Gauri P. Misra, Thomas W. Gardner, and Tao L. Lowe
13 Refillable Devices for Therapy of Ophthalmic Diseases ...................... 305
Alan L. Weiner
14 Targeted Drug Delivery to the Eye Enabled by Microneedles ............ 331
Samirkumar R. Patel, Henry F. Edelhauser,
and Mark R. Prausnitz
Ocular Iontophoresis .............................................................................. 361
15
Francine F. Behar-Cohen, Peter Milne, Jean-Marie Parel,
and Indu Persaud
16 Drug and Gene Therapy Mediated by Physical Methods ................... 391
John M. Nickerson and Jeffrey H. Boatright
17 Protein Drug Delivery and Formulation Development ....................... 409
Rinku Baid, Puneet Tyagi, Shelley A. Durazo,
and Uday B. Kompella
18 Drug Suspension Development for the Back of the Eye ...................... 449
Jithan Aukunuru, Puneet Tyagi, Chandrasekar Durairaj,
and Uday B. Kompella
19 Regulatory Considerations in Product Development
for Back of the Eye .................................................................................. 469
Ashutosh A. Kulkarni
20 Clinical Endpoints for Back of the Eye Diseases .................................. 485
Karl G. Csaky
21 Druggable Targets and Therapeutic Agents for Disorders
of the Back of the Eye ............................................................................. 495
Robert I. Scheinman, Sunil K. Vooturi, and Uday B. Kompella
22 Development of Bile Acids as Anti-Apoptotic
and Neuroprotective Agents in Treatment of Ocular Disease ............. 565
Stephanie L. Foster, Cristina Kendall, Allia K. Lindsay,
Alison C. Ziesel, Rachael S. Allen, Sheree S. Mosley,
Esther S. Kim, Ross J. Molinaro, Henry F. Edelhauser,
Machelle T. Pardue, John M. Nickerson,
and Jeffrey H. Boatright
Index ................................................................................................................. 577
Contributors
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Rachael S. Allen, MS Department of Ophthalmology,
Emory University School of Medicine, Atlanta, GA, USA
Hari Krishna Ananthula, MS Division of Pharmaceutical Sciences,
University of Missouri-Kansas City, School of Pharmacy, Kansas City, MO, USA
Jithan Aukunuru, PhD Mother Teresa College of Pharmacy, Hyderabad, India
Rinku Baid, B.Pharm Nanomedicine and Drug Delivery Laboratory,
University of Colorado, Aurora, CO, USA
Francine F. Behar-Cohen, MD, PhD Université Paris Descartes,
Assistance Publique Hôpitaux de Paris, Paris, France
Jeffrey H. Boatright, PhD Department of Ophthalmology,
Emory University School of Medicine, Atlanta, GA, USA
Karl G. Csaky, MD, PhD Sybil Harrington Molecular Laboratory,
Retina Foundation of the Southwest, Dallas, TX, USA
Chandrasekar Durairaj, PhD
University of Colorado, Aurora, CO and Allergan, Inc., Irvine, CA, USA
Shelley A. Durazo, BS Nanomedicine and Drug Delivery Laboratory,
University of Colorado, Aurora, CO, USA
Henry F. Edelhauser, PhD Emory University Eye Center, Emory University,
Atlanta, GA, USA
Stephanie L. Foster Department of Ophthalmology,
Emory University School of Medicine, Atlanta, GA, USA
Thomas Gadek, PhD OphthaMystic Consulting, Oakland, CA, USA
Vadivel Ganapathy, PhD Department of Biochemistry and Molecular Biology,
Medical College of Georgia, Augusta, GA, USA
Nanomedicine and Drug Delivery Laboratory,
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