Delivery Technologies for Biopharmaceuticals : Peptides, Proteins, Nucleic Acids and Vaccines

個数:

Delivery Technologies for Biopharmaceuticals : Peptides, Proteins, Nucleic Acids and Vaccines

  • 在庫がございません。海外の書籍取次会社を通じて出版社等からお取り寄せいたします。
    通常6~9週間ほどで発送の見込みですが、商品によってはさらに時間がかかることもございます。
    重要ご説明事項
    1. 納期遅延や、ご入手不能となる場合がございます。
    2. 複数冊ご注文の場合、分割発送となる場合がございます。
    3. 美品のご指定は承りかねます。
  • ≪洋書のご注文につきまして≫ 「海外取次在庫あり」および「国内仕入れ先からお取り寄せいたします」表示の商品でも、納期の目安期間内にお届けできないことがございます。あらかじめご了承ください。

  • 製本 Hardcover:ハードカバー版/ページ数 421 p.
  • 言語 ENG
  • 商品コード 9780470723388
  • DDC分類 615.6

Full Description


Successful delivery of biopharmaceuticals is a major challenge because their molecular properties lead to poor physical and chemical stability in the body and limited membrane permeability. Delivery Technologies for Biopharmaceuticals is the first single-volume reference to describe the strategies to overcome the main barriers for successful delivery of all major classes of biopharmaceuticals--peptides, proteins, nucleic acids, and vaccines. With extensive case studies showing how the science has been put into practice, this essential introduction will be of value to researchers and students working in drug delivery, formulation, biopharmaceuticals, medicinal chemistry, and new materials development.

Table of Contents

Preface                                            xv
List of Contributors xvii
INTRODUCTION 1
1. Challenges in Delivery of 3
Biopharmaceuticals; the Need for Advanced
Delivery Systems
Hanne M ck Nielsen and Lene Jorgensen
1.1 Introduction 3
1.2 Overcoming Delivery Barriers 4
1.2.1 Stabilization 4
1.2.2 Enhancing Delivery 5
1.3 Drug Delivery Technologies and 5
Excipients
1.4 Risks 6
1.5 Conclusion 7
References 7
DELIVERY OF BIOPHARMACEUTICALS 9
2. Novel Formulation Approaches for Peptide 11
and Protein Injectables
Mingshi Yang and Sven Frokjaer
2.1 Introduction 11
2.2 Formulation Challenges 12
2.3 Chemical Modification of Proteins and 13
Peptides
2.3.1 PEGylation 13
2.3.2 Glycoengineering 15
2.3.3 Acylation 16
2.3.4 Amino Acid Substitution 17
2.3.5 Protein Fusion 17
2.4 Depot Delivery Systems 18
2.4.1 Micro- and Nanoparticulate Systems 18
2.4.2 In Situ Depot-Forming Systems 21
2.4.3 Implant Systems 21
2.5 Other Delivery Systems 22
2.5.1 Protein Crystallization and/or 22
Precipitation
2.5.2 Injection Devices 22
2.6 Conclusions 23
References 23
3. Novel Non-Injectable Formulation 29
Approaches of Peptides and Proteins
Shirui Mao, Dongmei Cun and Yoshiaki
Kawashima
3.1 Introduction 29
3.2 Intranasal Delivery of 30
Peptide/Protein Drugs
3.2.1 Properties of Intranasal Delivery 30
3.2.2 Strategies to Enhance Intranasal 31
Absorption
3.3 Pulmonary Delivery of Peptide/Protein 36
Drugs
3.3.1 Properties of Pulmonary Delivery 36
3.3.2 Strategies to Enhance Pulmonary 36
Delivery
3.4 Buccal Administration of 42
Peptide/Protein Drugs
3.4.1 Properties of Buccal Delivery 42
3.4.2 Strategies to Improve Buccal 44
Absorption
3.5 Oral Delivery of Peptide/Protein Drugs 47
3.5.1 Challenges of Oral Delivery 47
3.5.2 Strategies to Enhance Oral 48
Absorption
3.6 Transdermal Delivery of 53
Peptide/Protein Drugs
3.6.1 Properties of Transdermal Delivery 53
3.6.2 Strategies to Improve Transdermal 53
Absorption of Proteins/Peptides
3.7 Conclusions 56
References 57
4. Chemical Vectors for Delivery of Nucleic 69
Acid-Based Drugs
Elizabeth A. Vasievich and Leaf Huang
4.1 Introduction 69
4.2 Barriers to Delivery of Nucleic Acids 70
4.2.1 Anatomical 70
4.2.2 Cellular 70
4.3 Major Classes of Delivery Vectors 71
4.3.1 Introduction 71
4.3.2 Cationic Lipids 71
4.3.3 Cationic Polymers 73
4.3.4 Cationic Dendrimers 74
4.3.5 Cell Penetrating Peptides (CPP) 75
and DNA Mimics
4.3.6 Naked DNA 76
4.4 Targeted Delivery 76
4.4.1 Introduction 76
4.4.2 Targeting Solid Tumours and/or 77
Metastasis
4.5 Triggered Release 79
4.5.1 Introduction 79
4.5.2 Proton Sponge Effect 80
4.5.3 Magnetofection (Magnetic 80
Delivery)
4.5.4 Hyperthermic Delivery 81
4.5.5 Reductive Agents 82
4.5.6 Biotin泡vidin 82
4.5.7 Electrochemical 83
4.6 Recent Clinical Trials Using Naked 83
and Chemically Complexed Nucleic Acids
4.6.1 Introduction 83
4.6.2 Naked Nucleic Acids in Clinical 83
Trials
4.6.3 Lipid-Based Nucleic Acid Carriers 85
in Clinical Trials
4.6.4 Polymer-Based Nucleic Acid 86
Carriers in Clinical Trials
4.7 Conclusion 86
References 87
5. Viral Technology for Delivery of Nucleic 93
Acids
Shervin Bahrami and Finn Skou Pedersen
5.1 Introduction 93
5.2 Barriers and Topological Requirements 95
to Cellular Entry
5.2.1 Enveloped Viruses and Membrane 95
Fusion
5.2.2 Non-Enveloped Viruses 97
5.3 Routes of Administration 98
5.4 Delivery Vector Requirements 98
5.4.1 Targeting 98
5.4.2 Expression 100
5.4.3 Safety 101
5.5 Examples of Viral Delivery Technology 103
5.5.1 Retroviral and Lentiviral Vectors 103
5.5.2 Adenovirus Vectors 105
5.5.3 Adeno-Associated Virus Vectors 106
5.5.4 Mixed Delivery Systems 107
5.5.5 In Vitro Assembled Delivery 108
Vehicles
5.6 Conclusion 108
References 109
6. The Innate Immune Responses, Adjuvants 113
and Delivery Systems
S. Moein Moghimi
6.1 Introduction 113
6.2 Dendritic Cell Immunobiology 117
6.3 Antigen Capture 119
6.4 Particulate Antigen Delivery Systems 120
6.5 Signalling Receptors and the Role of 121
Adjuvants
6.6 Conclusions 123
References 124
DELIVERY TECHNOLOGIES FOR BIOPHARMACEUTICALS 129
7. Lipid Nanoparticle-Based Systems for 131
Delivery of Biomacromolecule Therapeutics
Susana Martins, Domingos C. Ferreira and
Eliana B. Souto
7.1 Introduction 131
7.2 Definitions and Properties of Solid 133
Lipid Nanoparticles (SLNs)
7.3 Definitions and Properties of 135
Lipid-Drug Conjugates (LDCs)
7.4 Administration, Delivery and Targeting 136
7.5 Toxicity and Safety 138
7.6 Applications for Biopharmaceuticals 139
7.6.1 Peptides and Proteins 139
7.6.2 Nucleic Acids 139
7.6.3 Vaccines 142
7.7 Conclusions 142
References 142
8. Dendrimers in Delivery of 149
Biopharmaceuticals
Chandan Thomas and Fakhrul Ahsan
8.1 Introduction 149
8.1.1 Properties of Dendrimers as a 150
Carrier System
8.2 Case I  Application of Dendrimers in 153
Delivery of Large Molecular Weight Drugs
8.3 Case II  Application of Dendrimers 155
in Gene Delivery
8.3.1 Case IIA  Application of 156
PAMAM-PLGA Microparticle Conjugates in
Gene Delivery
8.3.2 Case BB  Application of 158
Dendrimers in siRNA Delivery
8.4 Case D1  Application of Dendrimers 162
in Vaccine Delivery
8.5 Concluding Remarks 165
References 166
PEPTIDES AND PROTEINS 169
9. Modification of Peptides and Proteins 171
Susanne Hostrup, Kasper Huus and Henrik
Parshad
9.1 Introduction 171
9.2 PEGylated Peptides and Proteins 171
9.2.1 Methods 172
9.2.2 Conceptual Considerations on 173
PEGylation
9.2.3 Pharmacokinetic Aspects 174
9.2.4 Pharmaceutical Aspects 175
9.2.5 PEGylated Proteins in Advanced 177
Delivery Systems
9.3 Lipidization of Peptides and Proteins 177
9.3.1 Methods of Lipidization 177
9.3.2 Conceptual Considerations on 178
Lipidization
9.3.3 Improved Pharmacokinetics 178
9.3.4 Improved Delivery via 179
Non-Parenteral Delivery Routes
9.3.5 Pharmaceutical Aspects 180
9.3.6 Lipidization in Advanced Delivery 181
Systems
9.4 Modification of the Primary Structure 181
of Peptides and Proteins
9.4.1 Strategies for Designing Protein 182
Analogues
9.4.2 Advantages and Disadvantages 183
9.4.3 Pharmaceutical Aspects萌eneral 183
Principles for Improving Protein
Stability
9.4.4 Pharmacokinetic Aspects 185
9.4.5 Manipulating the Isoelectrical 185
Point (pI) by Molecular Engineering
9.5 General Considerations on Processing 186
and Characterization
9.6 Conclusions 186
References 187
10. Nanocarriers for the Delivery of Peptides 193
and Proteins
Kenneth Lundstrom
10.1 Introduction 193
10.2 Polymeric Nanoparticles 194
10.2.1 Lactic/Glycotide Polymers 194
10.2.2 Polycaprolactones 195
10.2.3 Polyphosphoesters 195
10.2.4 Polyanhydrides 196
10.2.5 Polyorthoesters 196
10.2.6 Block Copolymers with a Specific 197
Emphasis on Medusa
10.2.7 Cross-Linked Dextran 198
10.3 In Situ Depot Forming Systems 199
10.3.1 Precipitation Systems 199
10.3.2 Thermal Gelling Systems 199
10.3.3 Cross-Linked Systems 200
10.3.4 Thermoplastic Semisolids 201
10.4 Conclusions 202
References 202
11. Polymer-Based Delivery Systems for Oral 207
Delivery of Peptides and Proteins
Bruno Sarmento, Domingos Ferreira and
Te ilo Vasconcelos
11.1 Introduction 207
11.2 Advances in Oral Protein Delivery 208
11.3 Intestinal Considerations for 209
Protein Absorption
11.4 Polymer-Based Delivery Systems for 211
Oral Delivery of Proteins
11.4.1 Hydrogels 211
11.4.2 Patches and Tablets 212
11.4.3 Microparticles 213
11.4.4 Nanoparticles 215
11.5 Conclusions 219
References 220
12. Advanced Pulmonary Delivery of Peptides 227
or Proteins Using Polymeric Particles
Yu Seok Youn, Kang Choon Lee, You Han Bae,
Kun Na and Eun Seong Lee
12.1 Introduction 227
12.2 Practical Issues in the Pulmonary 228
Delivery of Peptides and Proteins
12.2.1 Physiological Features of the 228
Lungs
12.2.2 Barriers to the Pulmonary 228
Delivery of Peptides and Proteins
12.2.3 Factors Affecting the Pulmonary 230
Delivery of Peptide and Protein
Particles
12.3 Polymeric Microparticles for 231
Delivering Peptides and Proteins
12.4 Porous Microparticles 232
12.5 Polymeric Nanoparticles 237
12.6 Sustained or Controlled Release 239
Issues in Polymeric Particle Formulations
12.7 Stability Issues of Peptides and 240
Proteins in Particles
12.8 Toxicity Issues of Inhaled Particles 240
12.9 Conclusions 240
References 241
NUCLEIC ACIDS 245
13. Polymer Microparticles for Nucleic Acid 247
Delivery
Tim Pearce, Jared Hierman and Chun Wang
13.1 Introduction 247
13.2 Microparticles Based on 248
Poly(Lactic-co-Glycolic Acids) (PLGA)
13.2.1 Overview 248
13.2.2 Design Parameters 248
13.2.3 General Strategies and 251
Fabrication of Microparticles
13.2.4 Optimization of Microparticle 253
Formulations
13.2.5 Combining Polycations with PLGA 254
Microparticles
13.2.6 Current Applications 256
13.3 Other Types of Polymer Microparticles 257
13.3.1 Alginate 257
13.3.2 Chitosan 258
13.3.3 Hyaluronan (HA) 259
13.3.4 Macro-Albumin Aggregates (MAA) 260
13.3.5 260
Poly(D,L-Lactide-co-4-Hydroxy-L-Proline)
(PLHP)
13.3.6 The Pluronics 261
13.3.7 Poly(Ortho Esters) (POEs) 262
13.3.8 Polyacrylamide 263
13.4 Conclusions 263
References 264
14. Pulmonary Delivery of Small Interfering 269
RNA for Novel Therapeutics
Qing Ge, David Evans, John J. Xu, Harry H.
Yang and Patrick Y. Lu
14.1 Introduction 269
14.2 RNA Interference: Mechanism of Action 270
14.3 Lung Physiology 270
14.4 Animal Models 272
14.5 siRNA Delivery to Treat Pulmonary 273
Diseases
14.5.1 Challenges 273
14.5.2 Viral Versus Non-Viral Vectors 274
14.5.3 Airway siRNA Delivery 275
14.5.4 Intravenous siRNA Delivery 278
14.5.5 Other Delivery Methods 279
14.6 siRNA-Induced Inflammatory Response 279
14.7 Case Studies 280
14.7.1 siRNA Therapeutics Against RSV 280
and PIV Infection in Mouse
14.7.2 siRNA Therapeutics for Treatment 281
of SCV Infection in Monkey
14.8 Faster Drug for Unknown Bugs 284
14.9 Conclusions 284
References 285
15. Lipid-Based Formulations for siRNA 291
Delivery
Camilla Foged, Pieter Vader and Raymond M.
Schiffelers
15.1 Introduction 291
15.2 Cationic Lipid-Based Delivery 292
Systems for Nucleic Acid-Based Drugs
15.2.1 Helper Lipids 293
15.2.2 Lipopolymers 294
15.2.3 Active Targeting 294
15.3 Neutral and Anionic Lipid-Based Drug 296
Delivery Systems
15.4 Mechanisms of Internalization 296
15.5 Immune Activation 297
15.6 Conclusions 299
References 300
16. Cellular Bioavailability of Peptide 305
Nucleic Acids (PNAs) Conjugated to Cell
Penetrating Peptides
Takehiko Shiraishi and Peter E. Nielsen
16.1 Introduction 305
16.2 Peptide Nucleic Acids (PNAs) 306
16.3 Cell Penetrating Peptides (CPPs) 306
16.4 Cellular Uptake Versus 307
Bioavailability
16.5 PNA Conjugates 307
16.6 Efficacy Versus Efficiency 307
16.7 Auxiliary Agents 330
16.8 In Vivo Activity of PNA Conjugates 331
16.9 Conclusions 331
References 336
17. DEAE-dextran-MMA Graft Copolymer for 339
Non-Viral Delivery of DNA
Yasuhiko Onishi, Yuki Eshita and Masaaki
Mizuno
17.1 Introduction 339
17.2 Theoretical 340
17.3 Materials and Methods 341
17.3.1 Preparation of DDMC 341
17.3.2 Characterization of DDMC 341
17.3.3 Reaction Between DDMC and DNA 341
17.3.4 The Structure of the Complex 343
Between DNA and DDMC
17.3.5 Transfection 345
17.3.6 Protection from DNase Degradation 350
17.3.7 DNA Delivery Pathways by DDMC 352
17.4 Conclusions 353
References 354
VACCINES 357
18. Liposomes in Adjuvant Systems for 359
Parenteral Delivery of Vaccines
Dennis Christensen, Karen Korsholm, Grith
Kr er Wood, Afzal Mohammed, Vincent
Bramwell, Peter Andersen, Else Marie Agger
and Yvonne Perrie
18.1 The Structural Basis of Liposomes 359
18.2 Key Characteristics Which Make 360
Liposomes Advantagous as Vaccine Delivery
Systems
18.3 Formulation Approaches to Improve 363
Adjuvanticity and Enhance Immunological
Targeting
18.3.1 Immunomodulators 364
18.3.2 Physicochemical Properties 365
18.4 Instability Considerations of 366
Liposomes
18.5 Techniques to Formulate Long-Term 368
Stable Liposome Formulations
18.5.1 Protection During Freeze-Drying 369
18.6 Conclusion 371
References 372
19. Influenza Virosomes as Delivery Systems 377
for Antigens
Mario Amacker, Stefan Moese, Andreas R.
Kammer, Ari Helenius and Rinaldo Zurbriggen
19.1 Introduction 377
19.1.1 Immune Stimulating Reconstituted 377
Influenza Virosomes (IRIVs) as Adjuvant
and Delivery System
19.1.2 Mechanisms of Action 379
19.2 A Case Study  Antigen-Virosome Drug 382
Delivery System
19.2.1 Particle Characterization 382
19.2.2 Virosome Uptake into HeLa Cells 382
19.2.3 Humoral Immune Response to 385
Antigen Virosomes
19.2.4 Cellular Immune Response to 386
Antigen Virosomes
19.2.5 Efficiency of the Antigen 388
Virosome Drug Delivery System
19.3 Methods 389
19.3.1 Virosome Formulation 389
19.3.2 Size Determination 389
19.3.3 Freeze芳racture Electron 389
Microscopy
19.3.4 Transmission Electron Microscopy 390
19.3.5 TIRF Microscopy 390
19.3.6 Mice and Immunizations 390
19.3.7 Intracellular IFNγ Staining 390
19.3.8 ELISA 391
References 391
20. GRAZAXョ: An Oromucosal Vaccine for 395
Treating Grass Pollen Allergy with
Immunotherapy
Annette R melmayer Lundegaard, Lise Lund
and J gen Nedergaard Larsen
20.1 Introduction 395
20.2 Specific Immunotherapy 396
20.3 Description of Grass Pollen Extract 397
20.4 Technologies of Fast Dissolving 398
Tablets
20.5 Formulation of GRAZAXョ 399
20.6 Production of GRAZAXョ 400
20.7 Specifications and Analytical 401
Procedures
20.7.1 Physical and Chemical Tests 401
20.7.2 Immunochemical Tests 402
20.7.3 Microbial Tests 403
20.8 Feasibility Study: Additional 403
Analyses
20.9 Conclusions 403
References 404
FINAL COMMENTS 405
21. Delivery Technologies for 407
Biopharmaceuticals: A Critical Assessment
Marco van de Weert
21.1 Introduction 407
21.2 Large Scale Production and 408
Reproducibility
21.3 Safety Concerns 408
21.4 Cost唯enefit Ratio 410
21.5 Conclusion 410
References 411
Index 413