Oral Delivery of Macromolecular Drugs Barriers, Strategies and Futur

Due to a rapid development in biotechnology more and more macromolecular drugs such as therapeutic peptides, oligosaccharides and nucleic acids are entering the pharmaceutical arena representing unprecedented challenges from the drug delivery point of vie

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Oral Delivery of Macromolecular Drugs Barriers, Strategies and Future Trends

Oral Delivery of Macromolecular Drugs

Andreas Bernkop-Schnu¨rch Editor

Oral Delivery of Macromolecular Drugs Barriers, Strategies and Future Trends

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Editor Andreas Bernkop-Schnu¨rch Universita¨t Innsbruck Fakulta¨t fu¨r Chemie und Pharmazie Inst. Pharmazie Innrain 52, 6020 Innsbruck, Austria [email protected]

ISBN 978-1-4419-0199-6 e-ISBN 978-1-4419-0200-9 DOI 10.1007/978-1-4419-0200-9 Springer Dordrecht Heidelberg London New York Library of Congress Control Number: 2009929310 # Springer ScienceþBusiness Media, LLC 2009 All rights reserved. This work may not be translated or copied in whole or in part without the written permission of the publisher (Springer ScienceþBusiness 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 ScienceþBusiness Media (www.springer.com)

Preface

Due to a rapid development in biotechnology more and more macromolecular drugs such as therapeutic peptides, oligosaccharides and nucleic acids are entering the pharmaceutical arena representing unprecedented challenges from the drug delivery point of view. One of the likely greatest challenges is their oral administration presenting a series of attractive advantages. These advantages are in particular of high relevance for the treatment of pediatric patients and include the avoidance of additional risks, pain and discomfort associated with injections. Furthermore, oral formulations are less expensive to produce, as they do not need to be manufactured under sterile conditions. The oral administration is by far the most favored one. The majority (84%) of 50 most-sold pharmaceutical products in US and Europe markets are given orally. Although there have been major advances in delivering macromolecular drugs in humans by other non-invasive routes, including the pulmonary delivery of insulin, we did so far not succeed in the development of oral delivery systems for these therapeutic agents. Apart from a few exceptions such as ciclosporin, desmopressin, chondroitin sulphate and bromelain macromolecular drugs cannot be administered orally. The de