Format:
Online-Ressource (digital)
ISBN:
9781441902009
Series Statement:
SpringerLink
Content:
Recent and rapid progress in the field of biotechnology has resulted in an increasing number of novel macromolecular drugs with great promise for further advanced research and clinical application. However, the delivery of these macromolecular drugs by routes other than the parenteral route is difficult. The pipeline of macromolecular drugs derived from biotechnology presents a challenging opportunity to develop practical dosage forms that could be dosed via the oral route. Given this, the successful oral delivery of macromolecular drugs presents an enormous opportunity. This volume will provide an overview of the innovative oral delivery technologies that have demonstrated success in human testing and will go on to cite the challenges, strategies, and future trends that are to be expected.
Note:
Description based upon print version of record
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Oral Delivery of Macromolecular Drugs; Preface; Contents; Contributors; About the Editor; Enzymatic Barriers; 1.1 Introduction; 1.2 The Peptidases; 1.3 The Nucleases; 1.4 Other Enzymes; 1.5 Where Are the Enzymes in the GI Tract?; 1.5.1 The Stomach; 1.5.2 The Lumen of the Small Intestine; 1.5.2.1 Pancreatic Enzymes; 1.5.2.2 Cellular Enzymes; 1.6 Quantitative Aspects of Intestinal Enzymes: How Much and How Active?; 1.7 The Colon; 1.8 The Importance of In Vitro Testing; 1.8.1 Strategies for In Vitro Testing of the Stability of Therapeutic Macromolecules and Macromolecular Formulations
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1.9 ConclusionsReferences; Gastrointestinal Mucus Gel Barrier; 2.1 Introduction; 2.2 Mucin Structural Properties; 2.2.1 Multi-domain Organization; 2.2.1.1 Mucin (O-Glycosylated) Domains; 2.2.1.2 CS-Domains; 2.2.1.3 D-Domains; 2.2.1.4 C- and CK-Domains; 2.2.2 Glycosylation; 2.2.2.1 O-Glycosylation; 2.2.2.2 N-Glycosylation; 2.2.2.3 C-Mannosylation; 2.2.3 Oligomerization/Multimerization; 2.2.4 Molecular Polydispersity; 2.3 Mucin Biosynthesis and Intracellular Processing; 2.3.1 Endoplasmic Reticulum; 2.3.2 Golgi Complex; 2.4 Mucin Intracellular Storage and Secretion; 2.4.1 Mucin Granule
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2.4.2 Mucin Granule Exocytosis2.4.2.1 Regulatory Aspects; 2.4.2.2 Biochemical/Biophysical Aspects; 2.5 Mucin Extracellular Organization; 2.5.1 Mucin Entanglements; 2.5.2 Other Interchain Links; 2.5.3 Mucinases; 2.5.4 Emerging Notion; 2.6 Other Mucus Components; 2.7 Diffusion of Macromolecules in Mucus; 2.7.1 Influence of Mesh Size; 2.7.2 Influence of Other Factors; 2.8 Conclusions; References; The Absorption Barrier; 3.1 Introduction; 3.2 Anatomy of the Digestive Tract; 3.3 Barriers to Transcellular Absorption; 3.3.1 Passive Diffusion; 3.3.2 Transporter Systems; 3.3.3 Pinocytosis
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3.3.4 Transport by Caveolae3.3.5 Efflux Systems; 3.4 Barriers to Paracellular Absorption; 3.4.1 The Tight Junctional Complex; 3.4.2 Modulation of Intestinal Tight Junctions; References; Strategies to Overcome the Enzymatic Barrier; 4.1 Introduction; 4.2 Formulations That Can Protect Drugs from Enzymatic Degradation; 4.3 Chemical Modification; 4.3.1 Modification of N and C Terminus; 4.3.2 Replacement of Labile Amino Acids; 4.3.3 PEGylation; 4.4 Enzyme Inhibitors; 4.4.1 Protease Inhibitors Which Are Not Based on Amino Acids
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4.4.2 Protease Inhibitors Which Are Based on Amino Acids and Modified Amino Acids4.4.3 Protease Inhibitors Which Are Based on Peptides and Modified Peptides; 4.4.4 Protease Inhibitors Which Are Based on Polypeptides; 4.4.5 Protease Inhibitors That Can Complex Ions; 4.4.6 Protease Inhibitors Based on Multifunctional Mucoadhesive Polymers; 4.4.6.1 Poly(acrylates); 4.4.6.2 Thiolated Polymers; 4.4.6.3 Polymer-Enzyme Inhibitor Conjugates; 4.5 Conclusion and Future Trends; References; Low Molecular Mass Permeation Enhancers in Oral Delivery of Macromolecular Drugs; 5.1 Introduction
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5.2 Transcellular Permeation Enhancers
Additional Edition:
ISBN 9781441901996
Additional Edition:
Buchausg. u.d.T. ISBN 978-1-441-90199-6
Language:
English
DOI:
10.1007/978-1-4419-0200-9
URL:
Volltext
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