Nanoparticulates as drug carriers:
Gespeichert in:
Format: | Buch |
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Sprache: | English |
Veröffentlicht: |
London
Imperial College Press
2006
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Schlagworte: | |
Online-Zugang: | Inhaltsverzeichnis |
Beschreibung: | XXIX, 724 S. Ill., graph. Darst. |
ISBN: | 1860946305 |
Internformat
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245 | 1 | 0 | |a Nanoparticulates as drug carriers |c ed. Vladimir P. Torchilin |
264 | 1 | |a London |b Imperial College Press |c 2006 | |
300 | |a XXIX, 724 S. |b Ill., graph. Darst. | ||
336 | |b txt |2 rdacontent | ||
337 | |b n |2 rdamedia | ||
338 | |b nc |2 rdacarrier | ||
650 | 4 | |a Biomedical materials | |
650 | 4 | |a Nanoparticles | |
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Datensatz im Suchindex
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adam_text | Contents
Contributors v
1. Introduction. Nanocarriers for Drug Delivery: Needs and Requirements 1
Vladimir Torchilin
References 6
2. Nanoparticle Flow: Implications for Drug Delivery 9
Alexander T. Florence
1 Introduction 9
2 Background 11
3 Studies on Nanoparticle Flow 13
4 Convection and Diffusion 13
5 Bifurcations 15
6 Interaction with Blood Constituents and Endogenous Molecules . . 16
7 Nanoparticles with Surface Ligands 18
8 Deposition on Surfaces and Attachment to Receptors in Flow
Conditions 18
9 Does Shape Matter? 20
10 Speculations on Flow and the EPR Effect 21
11 Intra tumoral Injection 22
12 Conclusions 23
References 24
3. Polymeric Nanoparticles as Drug Carriers and Controlled Release
Implant Devices 29
SM Moghimi, E Vega, ML Garcia, OAR Al Hanbali and KJ Rutt
1 Introduction 29
xiii
xiv Contents
2 Nanoparticle Engineering 30
2.1 Drug release mechanisms 32
3 Site specific Targeting with Nanoparticles: Importance of Size
and Surface Properties 33
4 Conclusions 37
References 38
4. Genetic Vaccines: A Role for Liposomes 43
Gregory Gregoriadis, Andrew Bacon, Brenda McCormack and Peter Laing
1 Introduction 43
2 The DNA Vaccine 44
3 DNA Vaccination via Liposomes 45
3.1 Procedure for the entrapment of plasmid DNA into
liposomes 46
3.2 DNA immunization studies 47
3.3 Induction of a cytotoxic T lymphocyte (CTL) response by
liposome entrapped plasmid DNA 50
4 The Co delivery Concept 51
References 53
5. Polymer Micelles as Drug Carriers 57
Elena V. Batrakova, Tatiana K. Bronich, Joseph A. Vetro and
Alexander V. Kabanov
1 Introduction 57
2 Polymer Micelle Structures 58
2.1 Self assembled micelles 58
2.2 Unimolecular micelles 61
2.3 Cross linked micelles 62
3 Drug Loading and Release 63
3.1 Chemical conjugation 63
3.2 Physical entrapment 64
3.3 Polyionic complexation 66
4 Pharmacokinetics and Biodistribution 68
5 Drug Delivery Applications 72
5.1 Chemotherapy of cancer 72
5.2 Drug delivery to the brain 76
5.3 Formulations of antifungal agents . 77
5.4 Delivery of imaging agents 77
5.5 Delivery of polynucleotides 78
Contents xv
6 Clinical Trials 79
7 Conclusions 79
References 80
6. Vesicles Prepared from Synthetic Amphiphiles — Polymeric Vesicles
and Niosomes 95
Ijeoma Florence Uchegbu and Andreas G. Schatzlein
1 Introduction 95
2 Polymeric Vesicles 96
2.1 Polymer self assembly 97
2.2 Polymers bearing hydrophobic pendant groups 98
2.3 Block copolymers 101
2.4 Preparing vesicles from self assembling polymers 102
2.5 Self assembling polymerizable monomers 103
3 Polymeric Vesicle Drug Delivery Applications 104
3.1 Drug targeting 104
3.2 Gene delivery 105
3.3 Responsive release 106
3.3.1 pH 106
3.3.2 Enzymatic 106
3.3.3 Magnetic 107
3.3.4 Oxygen 108
4 Non ionic Surfactant Vesicles (Niosomes) 108
4.1 Self assembly 108
4.2 Polyhedral vesicles and giant vesicles (Discomes) Ill
4.3 Vesicle preparation 113
5 Niosome Delivery Applications 113
5.1 Drug targeting 113
5.1.1 Anti cancer drugs 113
5.1.2 Anti infectives 115
5.1.3 Delivery to the brain 115
5.2 Topical use of niosomes 116
5.2.1 Transdermal 116
5.2.2 Ocular 116
5.3 Niosomal vaccines 116
5.4 Niosomes as imaging agents 117
6 Conclusions 117
References 117
xvi Contents
7. Recent Advances in Microemulsions as Drug Delivery Vehicles 125
M Jayne Lawrence and Warankanga Warisnoicharoen
1 Definition 125
1.1 Microemulsion versus an emulsion 125
1.2 Microemulsion versus a nanoemulsion 126
1.3 Microemulsions 128
1.4 Microemulsions, swollen micelles, micelles 129
1.5 Microemulsions and cosolvent systems 130
2 Microemulsions as Drug Delivery Systems 130
2.1 Self emulsifying drug delivery systems (SEDDS) 131
2.2 Related systems 133
2.2.1 Microemulsion gels 133
2.2.2 Double or multiple microemulsions 134
2.3 Processed microemulsion formulations 134
2.3.1 Solid state or dry emulsions 134
3 Formulation 135
3.1 Surfactants and cosurfactants 136
3.2 Oils 138
3.3 Characterization 139
4 Routes of Administration 139
4.1 Oral 139
4.1.1 Proteins and peptides 140
4.1.2 Other hydrophilic molecules 141
4.1.3 Hydrophobic drugs 142
4.2 Buccal 144
4.3 Parenteral 144
4.3.1 Long circulating microemulsions 147
4.3.2 Targeted delivery 148
4.4 Topical delivery 148
4.4.1 Dermal and transdermal delivery 148
4.5 Ophthalmic 154
4.6 Vaginal 156
4.7 Nasal 157
4.8 Pulmonary 158
4.8.1 Antibacterials 159
5 Conclusion 160
References 160
Contents xvii
8. Lipoproteins as Pharmaceutical Carriers 173
Suwen Liu, Shining Wang and D. Robert Lu
1 Introduction 173
2 The Structure of Lipoproteins 174
3 Chylomicron as Pharmaceutical Carrier 175
4 VLDL as Pharmaceutical Carrier 176
5 LDL as Pharmaceutical Carrier 177
5.1 LDL as anticancer drug carriers 178
5.2 LDL as carriers for other types of bioactive compounds .... 179
5.3 LDL for gene delivery 179
6 HDL as Pharmaceutical Carriers 179
7 Cholesterol rich Emulsions (LDE) as Pharmaceutical Carriers .... 180
8 Concluding Remark 181
References 182
9. Solid Lipid Nanoparticles as Drug Carriers 187
Karsten Mader
1 Introduction: History and Concept of SLN 187
2 Solid Lipid Nanoparticles (SLN) Ingredients and Production .... 188
2.1 General ingredients 188
2.2 SLN preparation 189
2.2.1 High shear homogenization and ultrasound 189
2.3 High pressure homogenization (HPH) 189
2.4 Hot homogenization 190
2.5 Cold homogenization 190
2.5.1 SLN prepared by solvent emulsification /
evaporation 191
2.5.2 SLN preparations by solvent injection 191
2.5.3 SLN preparations by dilution of microemulsions or
liquid crystalline phases 192
2.6 Further processing 193
2.6.1 Sterilization 193
2.6.2 Drying by lyophilization, nitrogen purging and
spray drying 194
3 SLN Structure and Characterization 196
4 The Frozen Emulsion Model and Alternative SLN Models .... 200
5 Nanostructured Lipid Carriers (NLC) 201
6 Drug Localization and Release 202
xviii Contents
7 Administration Routes and In Vivo Data 203
8 Summary and Outlook 205
References 205
10. Lipidic Core Nanocapsules as New Drug Delivery Systems 213
Patrick Saulnier and Jean Pierre Benoit
1 Introduction 213
2 Lipidic Nanocapsule Formulation and Structure 215
2.1 Process 215
2.2 Influence of the medium composition 216
2.3 Structure and purification of the LNC by dialysis 217
2.4 Imagery techniques 218
3 Electrical and Biological Properties 219
3.1 Electro kinetic comportment 219
3.2 Evaluation of complement system activation 220
4 Pharmacokinetic Studies and Biodistribution 220
5 Drug Encapsulation and Release 222
5.1 Ibuprofene 222
5.2 Amiodarone 223
6 Conclusions 223
References 224
11. Lipid Coated Submicron Sized Particles as Drug Carriers 225
Evan C. linger, Reena Zutshi, Terry O. Matsunaga and Rajan Ramaswami
1 Technology 225
2 Ultrasound Contrast Agents 228
3 Sonothrombolysis 232
4 Clinical Studies 237
5 Blood Brain Barrier 239
6 Drug Delivery 242
6.1 Targeted bubbles 242
6.2 Targeted submicron sized droplets 244
7 Gene Delivery 245
8 Oxygen Delivery 247
9 Pulmonary Delivery 248
10 Conclusion 249
References 250
Contents xix
12. Nanocapsules: Preparation, Characterization and Therapeutic
Applications 255
Ruxandra Grefand Patrick Couvreur
1 Introduction 255
2 Preparation 257
2.1 Nanocapsules obtained by interfacial polymerization 257
2.1.1 Oil containing nanocapsules 257
2.1.2 Nanocapsules containing an acqueous core 259
2.2 Nanocapsules obtained from preformed polymers 261
3 Characterization 263
4 Drug Release 265
5 Applications 266
5.1 Oral route 266
5.2 Parenteral route 267
5.3 Ocular delivery 269
6 Conclusion 270
References 271
13. Dendrimers as Nanoparticulate Drug Carriers 277
S onke Svenson and Donald A. Tomalia
1 Introduction 277
2 Nanoscale Containers — Micelles, Dendritic Boxes, Dendrophanes,
and Dendroclefts 279
2.1 Dendritic micelles 279
2.2 Dendritic box (Nano container) 280
2.3 Dendrophanes and dendroclefts 282
3 Dendrimers in Drug Delivery 282
3.1 Cisplatin 283
3.2 Silver salts 285
3.3 Adriamycin, methotrexate, and 5 fluorouracil 285
3.4 Etoposide, mefenamic acid, diclofenac, and venlafaxine .... 286
3.5 Ibuprofen, indomethacin, nifedipine, naproxen, paclitaxel,
and methylprednisolone 287
3.6 Doxorubicin and camptothecin — self immolative dendritic
prodrugs 289
3.7 Photodynamic therapy (PDT) and boron neutron capture
therapy (BNCT) 291
xx Contents
4 Nano Scaffolds for Targeting Ligands 292
4.1 Folic acid 292
4.2 Carbohydrates 293
4.3 Antibodies and biotin avidin binding 294
4.4 Penicillins 295
5 Dendrimers as Nano Drugs 295
6 Routes of Application 296
7 Biocompatibility of Dendrimers 297
8 Conclusions 299
References 299
14. Drug Nanocrystals/Nanosuspensions for the Delivery of Poorly
Soluble Drugs 307
Rainer H. Miiller and Jens Uwe A. H. Junghanns
1 Introduction 307
2 Definitions 308
3 Physicochemical Properties of Drug Nanocrystals 309
3.1 Change of dissolution velocity 309
3.2 Saturation solubility 309
3.3 Does size really matter? 311
3.4 Effect of amorphous particle state 312
4 Production Methods 313
4.1 Precipitation methods 313
4.1.1 Hydrosols 313
4.1.2 Amorphous drug nanoparticles (NanoMorph®) . . . .313
4.2 Homogenization methods 314
4.2.1 Microfluidizer technology 314
4.2.2 Piston gap homogenization in water (Dissocubes®) . . 314
4.2.3 Nanopure technology 315
4.3 Combination Technologies 315
4.3.1 Microprecipitation™ and High Shear Forces
(NANOEDGE™) 315
4.3.2 Nanopure® XP technology 316
5 Application Routes and Final Formulations 317
5.1 Oral administration 317
5.2 Parenteral administration 319
5.3 Miscellaneous administration routes 321
6 Nanosuspensions as Intermediate Products 322
Contents xxi
7 Perspectives 324
References 324
15. Cells and Cell Ghosts as Drug Carriers 329
Jose M. Lanao and M. Luisa Sayalero
1 Introduction 329
2 Bacterial Ghosts 329
2.1 Application of bacterial ghosts as a delivery system 331
3 Erythrocyte Ghosts 333
3.1 Applications of erythrocyte ghosts as a delivery system .... 335
4 Stem Cells 338
5 Polymorphonuclear Leucocytes 340
6 Apoptopic Cells 340
7 Tumor Cells 340
8 Dendritic Cells 341
9 Conclusions 341
References 342
16. Cochleates as Nanoparticular Drug Carriers 349
Leila Zarif
1 Introduction 349
2 Cochleates Nanoparticles in Oral Delivery 350
2.1 Cochleate structure 350
2.2 Cochleate preparation 350
2.2.1 Which phospholipid and which cation to use? 350
2.2.2 Which molecules can be entrapped in cochleates
nanoparticles 352
2.2.3 Multiple ways of preparing cochleates 353
2.3 Cochleates as oral delivery system for antifungal agent,
amphotericin B 355
2.3.1 In candidiasis animal model 355
2.3.2 In aspergillosis animal model 355
2.3.3 In cryptococcal meningitis animal model 357
2.3.4 Toxicity of amphotericin B cochleates 357
2.3.5 Pharmacokinetics of amphotericin B cochleates .... 357
2.4 Other potential applications for cochleates 359
2.4.1 Cochleate for the delivery of antibiotics 359
2.4.2 Delivery of clofazimine 360
xx ii Contents
2.4.3 Delivery of tobramycin 360
2.4.4 Cochleate for the delivery of anti inflammatory
drugs 361
2.5 Other uses of cochleates 361
3 Conclusion 361
References 362
17. Aerosols as Drug Carriers 367
N. Renee Labiris, Andrew P. Bosco and Myrna B. Dolovich
1 Introduction 367
2 Pulmonary Drug Delivery Devices 369
2.1 Nebulizers 369
2.2 Metered dose inhalers 371
2.3 Dry powder inhalers 373
3 Aerosol Particle Size 373
4 Targeting Drug Delivery in the Lung 376
5 Clearance of Particles from the Lung 378
5.1 Airway geometry and humidity 378
5.2 Lung clearance mechanisms 379
6 Nanoparticle Formulations for Inhalation 381
6.1 Diagnostic imaging 382
6.2 Vaccine delivery 383
6.3 Anti Tuberculosis therapy 385
6.4 Gene therapy 386
7 Conclusion 388
References 388
18. Magnetic Nanoparticles as Drug Carriers 397
Urs O. Hafeli and Mathieu Chastellain
1 Introduction 397
2 Definitions 398
2.1 Properties of magnetic materials 398
2.2 Nanoparticles 400
3 Magnetic Nanoparticles 401
3.1 Iron oxide based magnetic nanoparticles 401
3.2 Cobalt based magnetic nanoparticles 402
3.3 Iron based magnetic particles 402
3.4 Encapsulated magnetic nanoparticles 403
3.5 Biocompatibility issues of magnetic nanoparticles 403
Contents xxiii
4 Application of Magnetic Nanoparticles as Drug Carriers 404
4.1 Magnetic hyperthermia 405
4.2 Magnetic chemotherapy 406
4.3 Other magnetic treatment approaches 408
4.4 Magnetic gene transfer 409
5 Conclusions 410
References 411
19. DQAsomes as Mitochondria Specific Drug and DNA Carriers 419
Volkmar Weissig
1 Introduction 419
2 The Self Assembly Behavior of Bis Quinolinium Derivatives 420
2.1 Monte Carlo computer simulations 420
2.2 Physico chemical characterization 421
2.3 Structure activity relationship studies 422
3 DQAsomes as Mitochondrial Transfection Vector 424
4 DQAsomes as Carriers of Pro apoptotic Drugs 429
5 Summary 432
References 432
20. Liposomal Drug Carriers in Cancer Therapy 437
Alberto A. Gabizon
1 Introduction 437
2 The Challenge of Cancer Therapy 439
3 The Rationale for the Use of Liposomal Drug Carriers in Cancer . . 442
4 Liposome Formulation and Pharmacokinetics — Stealth
Liposomes 445
5 Preclinical Observations with Liposomal Drug Carriers
in Tumor Models 448
6 Liposomal Anthracyclines in the Clinic 449
6.1 Doxil 450
6.2 Myocet 454
6.3 Daunoxome 454
7 Clinical Development of Other Liposome entrapped
Cytotoxic Agents 455
8 The Future of Liposomal Nanocarriers 456
References 457
xxiv Contents
21. Nanoparticulate Drug Delivery to the Reticuloendothelial System
and to Associated Disorders 463
Mukul Kumar Basu and Sanchaita Lala
1 Introduction 463
2 Reticuloendothelial System and Associated Disorders 464
3 Uptake of Nanoparticles by the Reticuloendothelial System 464
3.1 Sites of uptake 464
3.2 Mechanism of uptake 465
3.3 Factors influencing uptake 468
3.4 Role of surface modifications on uptake 469
4 Active Targeting of Nanoparticles by Receptor Mediated
Endocytosis 471
5 Application in Chemotherapy 473
6 Summary 475
References 477
22. Delivery of Nanoparticles to the Cardiovascular System 481
Ban An Khazv
1 Introduction 481
2 Targeting the Myocardium with Immunoliposomes 481
3 Other Nanoparticle Targeting of the Cardiovascular System 484
4 Novel Application of Nano Immunoliposomes 485
5 CSIL as Targeted Gene or Drug Delivery 492
6 Conclusion 495
References 496
23. Nanocarriers for the Vascular Delivery of Drugs to the Lungs 499
Thomas Dziubla and Vladimir Muzykantov
1 Introduction 500
2 Biomedical Aspects of Drug Delivery to Pulmonary Vasculature . . 500
2.1 Routes for pulmonary drug delivery: Intratracheal vs
vascular 501
2.2 Pulmonary vasculature as a target for drug delivery 501
3 Pulmonary Targeting of Nanocarriers 503
3.1 Effects of carrier size on circulation and tissue distribution . . 503
Contents xxv
3.2 Passive targeting 505
3.2.1 Mechanical retention 505
3.2.2 Charge mediated retention and non viral gene
delivery 506
3.2.3 Pulmonary enhanced permeation retention (EPR)
effect 507
3.3 Active targeting 507
4 Carrier Design 509
4.1 Biocompatibility 509
4.2 Material selection (by application) 510
4.2.1 Imaging 510
4.2.2 Gene delivery 510
4.2.3 Delivery of therapeutic enzymes 511
4.2.4 Small molecule drugs 512
4.3 Types of nanocarriers 512
4.4 Mechanisms of drug loading 512
4.5 Drug release mechanisms 515
4.6 Nanocarriers for active targeting 516
5 Conclusion: Safety Issues, Limitations and Perspectives 517
References 518
24. Nanoparticulate Carriers for Drug Delivery to the Brain 527
Jorg Kreuter
1 Introduction 527
2 Nanoparticles 528
3 Biodistribution 530
3.1 Influence of surfactants on the biodistribution of
nanoparticles 530
3.2 Influence of PEGylation on the biodistribution of
nanoparticles 532
4 Pharmacology 534
5 Brain Tumors 536
6 Toxicology 538
7 Mechanism of the Delivery of Drug Across the Blood Brain
Barrier with Nanoparticles 539
8 Summary 541
9 Conclusions 542
References 542
xxvi Contents
25. Nanoparticles for Targeting Lymphatics 549
William Phillips
1 Introduction 549
1.1 The lymphatic vessels 550
1.2 Lymph nodes 551
2 Potential for Nanoparticles for Drug Delivery to Lymphatics .... 553
3 Importance of Lymph Nodes for Disease Spread and
Potential Applications of Lymph Node Drug Delivery 554
3.1 Cancer 554
3.2 HIV 555
3.3 Filaria 555
3.4 Anthrax 556
3.5 Tuberculosis 556
3.6 Importance of lymph node antigen delivery for development
of an immune response 557
4 Factors Influencing Nanoparticle Delivery to Lymph Nodes 559
4.1 Nanoparticle size 559
4.2 Nanoparticle surface 559
4.3 Effect of massage on lymphatic clearance of subcutaneously
injected liposomes 560
4.4 Macrophage phagocytosis 561
4.5 Fate of nanoparticles in lymph nodes 561
5 Nanoparticle Diagnostic Imaging Agents for Determining Cancer
Status of Lymph Nodes 561
5.1 Subcutaneous injection of iodinated nanoparticles for
computed tomography imaging 561
5.2 Subcutaneous and intraorgan injection of magnetic
resonance (MRI) contrast agents 563
5.3 Intravenous injection of magnetic nanoparticles for
MRI imaging 563
5.4 Nanoparticle diagnostic agents for localizing the sentinel
lymph node 565
5.5 Radiolabeled nanoparticles for sentinel lymph node
identification 566
5.6 mTc Colloidal nanoparticles for sentinel node identification . 566
5.7 Optical 568
5.8 Ultrasound nanobubbles 569
6 Recently Introduced Medical Imaging Devices for Monitoring
Lymph Node Delivery and Therapeutic Response 569
Contents xxvii
7 Nanoparticle Lymph Node Drug Delivery 571
7.1 Confusion in reporting lymph node delivery 571
7.2 Calculation of lymph node retention efficiency 573
8 Specific Types Nanoparticles for Lymph Node Targeting 573
8.1 PLGA nanoparticles 573
8.2 Micelles 574
8.3 Liposomes 574
9 Avidin Biotin Liposome Lymph Node Targeting Method 577
10 Massage and the Avidin Biotin Liposome Targeting Method 578
11 Nanoparticles for Lymph Node Anti Infectious Agent Delivery . . . 580
12 Liposomes for Intraperitoneal Lymph Node Drug Delivery 581
12.1 Intraperitoneal liposome encapsulated drugs 582
12.2 Effect of liposome size on intraperitoneal clearance 583
12.3 Avidin/Biotin liposome system for intraperitoneal and
lymph node drug delivery 584
12.4 Mediastinal lymph node drug delivery with avidin biotin
system by intrapleural injection 585
12.5 Avidin biotin for diaphragm and mediastinal lymph node
targeting 586
13 Nanoparticles for Cancer Therapy 587
13.1 Intralymphatic drug delivery to lymph nodes 587
13.2 Nanoparticles for treatment of metastatic lymph nodes of
upper GI malignacies 589
13.3 Lessons from endolymphatic radioisotope therapy 591
14 Advantages of Nanoparticles for Lymphatic Radiotherapy 592
15 Intraoperative Radiotherapy for Positive Tumor Margins
and for Treatment of Lymph Nodes 593
16 Potential of Using Radiolabeled Nanoparticles for Intratumoral
Radionuclide Therapy 593
17 Liposome Pharmacokinetics after Intratumoral Administration . . .595
18 Rhenium Labeled Liposomes for Tumor Therapy 595
19 Nanoparticles for Immune Modulation 597
20 Conclusions 598
References 598
26. Polymeric Nanoparticles for Delivery in the Gastro Intestinal Tract 609
Mayank D. Bhavsar, Dinesh B. Shenoy and Mansoor M. Amiji
1 Oral Drug Delivery 609
xxviii Contents
2 Anatomical and Physiological Considerations of Gastro intestinal
Tract (GIT) for Delivery 610
3 Introduction to Polymeric Nanoparticles as Carriers 614
4 Preparation of Polymeric Nanoparticles 615
5 Design Consideration for Nanoparticle based Delivery Systems . . 619
5.1 Polymer characteristics 619
5.2 Drug characteristics 620
5.3 Application characteristics 621
6 Nanoparticles in Experimental and Clinical Medicine 621
6.1 Drug delivery in the oral cavity 621
6.2 Gastric mucosa as a target for oral nanoparticle mediated
therapy 625
6.3 Nanoparticles for delivery of drugs and vaccines in the small
intestine 626
6.4 Nanoparticles for colon specific delivery 632
7 Integrating Polymeric Nanoparticles and Dosage Forms 634
8 Toxicology and Regulatory Aspects 636
8.1 Safety 637
8.2 Quality of material/characterization 638
8.3 Environmental considerations 638
9 Conclusion and Outlook 639
References 640
27. Nanoparticular Carriers for Ocular Drug Delivery 649
Alejandro Sanchez and Maria f. Alonso
1 Biopharmaceutical Barriers in Ocular Drug Delivery. Classification
of Nanoparticulate Carriers for Ocular Drug Delivery 650
2 Nanoparticulate Polymer Compositions as Topical Ocular Drug
Delivery Systems 651
2.1 First generation: Polymer nanoparticles and nanocapsules
for topical ocular drug delivery 652
2.1.1 Acrylic polymers based nanoparticles 654
2.1.2 Polyester based nanoparticles and nanocapsules . . .655
2.1.3 Polysaccharide based nanoparticles 657
2.2 Second nanoparticles generation: The coating approach .... 659
2.2.1 Polyacrylic coating 659
2.2.2 Polysaccharide coating 660
2.2.3 Polyethyleneglycol (PEG) coating 662
Contents xxix
2.3 Third nanoparticles generation: Towards functionalized
nanocarriers 663
3 Nanoparticulate Polymer Compositions as Subconjuctival Drug
Delivery Systems 665
4 Nanoparticulate Polymer Compositions as Intravitreal Drug
Delivery Systems 665
5 Conclusions and Outlook 667
References 668
28. Nanoparticles and Microparticles as Vaccine Adjuvants 675
Janet R. Wendorf, Manmohan Singh and Derek T. O Hagan
1 Introduction 675
2 Nanoparticle and Microparticle Preparation Methods 678
2.1 Nanoparticles and microparticles made from polyesters .... 678
2.2 Nanoparticles and microparticles made with chitosan 681
2.3 Other nanoparticles and microparticles 681
3 Adjuvant Effect of Nanoparticles and Microparticles 681
3.1 Nanoparticles and microparticles as mucosal adjuvants .... 682
3.2 Nanoparticles and microparticles as systemic adjuvants .... 686
4 Delivery of DNA Using Nanoparticles and Microparticles 688
5 Conclusions 690
References 691
29. Pharmaceutical Nanocarriers in Treatment and Imaging of Infection 697
Raymond M. Schiffelers, Gert Storm and Irma A. ]. M. Bakker Woudenberg
1 Introduction 697
2 Carriers that are Easily Recognized as Foreign Materials 698
3 Carriers that Avoid Recognition as Foreign Materials 701
4 Local Application of Carriers 705
5 Concluding Remarks 706
References 707
Index 713
|
adam_txt |
Contents
Contributors v
1. Introduction. Nanocarriers for Drug Delivery: Needs and Requirements 1
Vladimir Torchilin
References 6
2. Nanoparticle Flow: Implications for Drug Delivery 9
Alexander T. Florence
1 Introduction 9
2 Background 11
3 Studies on Nanoparticle Flow 13
4 Convection and Diffusion 13
5 Bifurcations 15
6 Interaction with Blood Constituents and Endogenous Molecules . . 16
7 Nanoparticles with Surface Ligands 18
8 Deposition on Surfaces and Attachment to Receptors in Flow
Conditions 18
9 Does Shape Matter? 20
10 Speculations on Flow and the EPR Effect 21
11 Intra tumoral Injection 22
12 Conclusions 23
References 24
3. Polymeric Nanoparticles as Drug Carriers and Controlled Release
Implant Devices 29
SM Moghimi, E Vega, ML Garcia, OAR Al Hanbali and KJ Rutt
1 Introduction 29
xiii
xiv Contents
2 Nanoparticle Engineering 30
2.1 Drug release mechanisms 32
3 Site specific Targeting with Nanoparticles: Importance of Size
and Surface Properties 33
4 Conclusions 37
References 38
4. Genetic Vaccines: A Role for Liposomes 43
Gregory Gregoriadis, Andrew Bacon, Brenda McCormack and Peter Laing
1 Introduction 43
2 The DNA Vaccine 44
3 DNA Vaccination via Liposomes 45
3.1 Procedure for the entrapment of plasmid DNA into
liposomes 46
3.2 DNA immunization studies 47
3.3 Induction of a cytotoxic T lymphocyte (CTL) response by
liposome entrapped plasmid DNA 50
4 The Co delivery Concept 51
References 53
5. Polymer Micelles as Drug Carriers 57
Elena V. Batrakova, Tatiana K. Bronich, Joseph A. Vetro and
Alexander V. Kabanov
1 Introduction 57
2 Polymer Micelle Structures 58
2.1 Self assembled micelles 58
2.2 Unimolecular micelles 61
2.3 Cross linked micelles 62
3 Drug Loading and Release 63
3.1 Chemical conjugation 63
3.2 Physical entrapment 64
3.3 Polyionic complexation 66
4 Pharmacokinetics and Biodistribution 68
5 Drug Delivery Applications 72
5.1 Chemotherapy of cancer 72
5.2 Drug delivery to the brain 76
5.3 Formulations of antifungal agents . 77
5.4 Delivery of imaging agents 77
5.5 Delivery of polynucleotides 78
Contents xv
6 Clinical Trials 79
7 Conclusions 79
References 80
6. Vesicles Prepared from Synthetic Amphiphiles — Polymeric Vesicles
and Niosomes 95
Ijeoma Florence Uchegbu and Andreas G. Schatzlein
1 Introduction 95
2 Polymeric Vesicles 96
2.1 Polymer self assembly 97
2.2 Polymers bearing hydrophobic pendant groups 98
2.3 Block copolymers 101
2.4 Preparing vesicles from self assembling polymers 102
2.5 Self assembling polymerizable monomers 103
3 Polymeric Vesicle Drug Delivery Applications 104
3.1 Drug targeting 104
3.2 Gene delivery 105
3.3 Responsive release 106
3.3.1 pH 106
3.3.2 Enzymatic 106
3.3.3 Magnetic 107
3.3.4 Oxygen 108
4 Non ionic Surfactant Vesicles (Niosomes) 108
4.1 Self assembly 108
4.2 Polyhedral vesicles and giant vesicles (Discomes) Ill
4.3 Vesicle preparation 113
5 Niosome Delivery Applications 113
5.1 Drug targeting 113
5.1.1 Anti cancer drugs 113
5.1.2 Anti infectives 115
5.1.3 Delivery to the brain 115
5.2 Topical use of niosomes 116
5.2.1 Transdermal 116
5.2.2 Ocular 116
5.3 Niosomal vaccines 116
5.4 Niosomes as imaging agents 117
6 Conclusions 117
References 117
xvi Contents
7. Recent Advances in Microemulsions as Drug Delivery Vehicles 125
M Jayne Lawrence and Warankanga Warisnoicharoen
1 Definition 125
1.1 Microemulsion versus an emulsion 125
1.2 Microemulsion versus a nanoemulsion 126
1.3 Microemulsions 128
1.4 Microemulsions, swollen micelles, micelles 129
1.5 Microemulsions and cosolvent systems 130
2 Microemulsions as Drug Delivery Systems 130
2.1 Self emulsifying drug delivery systems (SEDDS) 131
2.2 Related systems 133
2.2.1 Microemulsion gels 133
2.2.2 Double or multiple microemulsions 134
2.3 Processed microemulsion formulations 134
2.3.1 Solid state or dry emulsions 134
3 Formulation 135
3.1 Surfactants and cosurfactants 136
3.2 Oils 138
3.3 Characterization 139
4 Routes of Administration 139
4.1 Oral 139
4.1.1 Proteins and peptides 140
4.1.2 Other hydrophilic molecules 141
4.1.3 Hydrophobic drugs 142
4.2 Buccal 144
4.3 Parenteral 144
4.3.1 Long circulating microemulsions 147
4.3.2 Targeted delivery 148
4.4 Topical delivery 148
4.4.1 Dermal and transdermal delivery 148
4.5 Ophthalmic 154
4.6 Vaginal 156
4.7 Nasal 157
4.8 Pulmonary 158
4.8.1 Antibacterials 159
5 Conclusion 160
References 160
Contents xvii
8. Lipoproteins as Pharmaceutical Carriers 173
Suwen Liu, Shining Wang and D. Robert Lu
1 Introduction 173
2 The Structure of Lipoproteins 174
3 Chylomicron as Pharmaceutical Carrier 175
4 VLDL as Pharmaceutical Carrier 176
5 LDL as Pharmaceutical Carrier 177
5.1 LDL as anticancer drug carriers 178
5.2 LDL as carriers for other types of bioactive compounds . 179
5.3 LDL for gene delivery 179
6 HDL as Pharmaceutical Carriers 179
7 Cholesterol rich Emulsions (LDE) as Pharmaceutical Carriers . 180
8 Concluding Remark 181
References 182
9. Solid Lipid Nanoparticles as Drug Carriers 187
Karsten Mader
1 Introduction: History and Concept of SLN 187
2 Solid Lipid Nanoparticles (SLN) Ingredients and Production . 188
2.1 General ingredients 188
2.2 SLN preparation 189
2.2.1 High shear homogenization and ultrasound 189
2.3 High pressure homogenization (HPH) 189
2.4 Hot homogenization 190
2.5 Cold homogenization 190
2.5.1 SLN prepared by solvent emulsification /
evaporation 191
2.5.2 SLN preparations by solvent injection 191
2.5.3 SLN preparations by dilution of microemulsions or
liquid crystalline phases 192
2.6 Further processing 193
2.6.1 Sterilization 193
2.6.2 Drying by lyophilization, nitrogen purging and
spray drying 194
3 SLN Structure and Characterization 196
4 The "Frozen Emulsion Model" and Alternative SLN Models . 200
5 Nanostructured Lipid Carriers (NLC) 201
6 Drug Localization and Release 202
xviii Contents
7 Administration Routes and In Vivo Data 203
8 Summary and Outlook 205
References 205
10. Lipidic Core Nanocapsules as New Drug Delivery Systems 213
Patrick Saulnier and Jean Pierre Benoit
1 Introduction 213
2 Lipidic Nanocapsule Formulation and Structure 215
2.1 Process 215
2.2 Influence of the medium composition 216
2.3 Structure and purification of the LNC by dialysis 217
2.4 Imagery techniques 218
3 Electrical and Biological Properties 219
3.1 Electro kinetic comportment 219
3.2 Evaluation of complement system activation 220
4 Pharmacokinetic Studies and Biodistribution 220
5 Drug Encapsulation and Release 222
5.1 Ibuprofene 222
5.2 Amiodarone 223
6 Conclusions 223
References 224
11. Lipid Coated Submicron Sized Particles as Drug Carriers 225
Evan C. linger, Reena Zutshi, Terry O. Matsunaga and Rajan Ramaswami
1 Technology 225
2 Ultrasound Contrast Agents 228
3 Sonothrombolysis 232
4 Clinical Studies 237
5 Blood Brain Barrier 239
6 Drug Delivery 242
6.1 Targeted bubbles 242
6.2 Targeted submicron sized droplets 244
7 Gene Delivery 245
8 Oxygen Delivery 247
9 Pulmonary Delivery 248
10 Conclusion 249
References 250
Contents xix
12. Nanocapsules: Preparation, Characterization and Therapeutic
Applications 255
Ruxandra Grefand Patrick Couvreur
1 Introduction 255
2 Preparation 257
2.1 Nanocapsules obtained by interfacial polymerization 257
2.1.1 Oil containing nanocapsules 257
2.1.2 Nanocapsules containing an acqueous core 259
2.2 Nanocapsules obtained from preformed polymers 261
3 Characterization 263
4 Drug Release 265
5 Applications 266
5.1 Oral route 266
5.2 Parenteral route 267
5.3 Ocular delivery 269
6 Conclusion 270
References 271
13. Dendrimers as Nanoparticulate Drug Carriers 277
S'onke Svenson and Donald A. Tomalia
1 Introduction 277
2 Nanoscale Containers — Micelles, Dendritic Boxes, Dendrophanes,
and Dendroclefts 279
2.1 Dendritic micelles 279
2.2 Dendritic box (Nano container) 280
2.3 Dendrophanes and dendroclefts 282
3 Dendrimers in Drug Delivery 282
3.1 Cisplatin 283
3.2 Silver salts 285
3.3 Adriamycin, methotrexate, and 5 fluorouracil 285
3.4 Etoposide, mefenamic acid, diclofenac, and venlafaxine . 286
3.5 Ibuprofen, indomethacin, nifedipine, naproxen, paclitaxel,
and methylprednisolone 287
3.6 Doxorubicin and camptothecin — self immolative dendritic
prodrugs 289
3.7 Photodynamic therapy (PDT) and boron neutron capture
therapy (BNCT) 291
xx Contents
4 Nano Scaffolds for Targeting Ligands 292
4.1 Folic acid 292
4.2 Carbohydrates 293
4.3 Antibodies and biotin avidin binding 294
4.4 Penicillins 295
5 Dendrimers as Nano Drugs 295
6 Routes of Application 296
7 Biocompatibility of Dendrimers 297
8 Conclusions 299
References 299
14. Drug Nanocrystals/Nanosuspensions for the Delivery of Poorly
Soluble Drugs 307
Rainer H. Miiller and Jens Uwe A. H. Junghanns
1 Introduction 307
2 Definitions 308
3 Physicochemical Properties of Drug Nanocrystals 309
3.1 Change of dissolution velocity 309
3.2 Saturation solubility 309
3.3 Does size really matter? 311
3.4 Effect of amorphous particle state 312
4 Production Methods 313
4.1 Precipitation methods 313
4.1.1 Hydrosols 313
4.1.2 Amorphous drug nanoparticles (NanoMorph®) . . . .313
4.2 Homogenization methods 314
4.2.1 Microfluidizer technology 314
4.2.2 Piston gap homogenization in water (Dissocubes®) . . 314
4.2.3 Nanopure technology 315
4.3 Combination Technologies 315
4.3.1 Microprecipitation™ and High Shear Forces
(NANOEDGE™) 315
4.3.2 Nanopure® XP technology 316
5 Application Routes and Final Formulations 317
5.1 Oral administration 317
5.2 Parenteral administration 319
5.3 Miscellaneous administration routes 321
6 Nanosuspensions as Intermediate Products 322
Contents xxi
7 Perspectives 324
References 324
15. Cells and Cell Ghosts as Drug Carriers 329
Jose M. Lanao and M. Luisa Sayalero
1 Introduction 329
2 Bacterial Ghosts 329
2.1 Application of bacterial ghosts as a delivery system 331
3 Erythrocyte Ghosts 333
3.1 Applications of erythrocyte ghosts as a delivery system . 335
4 Stem Cells 338
5 Polymorphonuclear Leucocytes 340
6 Apoptopic Cells 340
7 Tumor Cells 340
8 Dendritic Cells 341
9 Conclusions 341
References 342
16. Cochleates as Nanoparticular Drug Carriers 349
Leila Zarif
1 Introduction 349
2 Cochleates Nanoparticles in Oral Delivery 350
2.1 Cochleate structure 350
2.2 Cochleate preparation 350
2.2.1 Which phospholipid and which cation to use? 350
2.2.2 Which molecules can be entrapped in cochleates
nanoparticles 352
2.2.3 Multiple ways of preparing cochleates 353
2.3 Cochleates as oral delivery system for antifungal agent,
amphotericin B 355
2.3.1 In candidiasis animal model 355
2.3.2 In aspergillosis animal model 355
2.3.3 In cryptococcal meningitis animal model 357
2.3.4 Toxicity of amphotericin B cochleates 357
2.3.5 Pharmacokinetics of amphotericin B cochleates . 357
2.4 Other potential applications for cochleates 359
2.4.1 Cochleate for the delivery of antibiotics 359
2.4.2 Delivery of clofazimine 360
xx ii Contents
2.4.3 Delivery of tobramycin 360
2.4.4 Cochleate for the delivery of anti inflammatory
drugs 361
2.5 Other uses of cochleates 361
3 Conclusion 361
References 362
17. Aerosols as Drug Carriers 367
N. Renee Labiris, Andrew P. Bosco and Myrna B. Dolovich
1 Introduction 367
2 Pulmonary Drug Delivery Devices 369
2.1 Nebulizers 369
2.2 Metered dose inhalers 371
2.3 Dry powder inhalers 373
3 Aerosol Particle Size 373
4 Targeting Drug Delivery in the Lung 376
5 Clearance of Particles from the Lung 378
5.1 Airway geometry and humidity 378
5.2 Lung clearance mechanisms 379
6 Nanoparticle Formulations for Inhalation 381
6.1 Diagnostic imaging 382
6.2 Vaccine delivery 383
6.3 Anti Tuberculosis therapy 385
6.4 Gene therapy 386
7 Conclusion 388
References 388
18. Magnetic Nanoparticles as Drug Carriers 397
Urs O. Hafeli and Mathieu Chastellain
1 Introduction 397
2 Definitions 398
2.1 Properties of magnetic materials 398
2.2 Nanoparticles 400
3 Magnetic Nanoparticles 401
3.1 Iron oxide based magnetic nanoparticles 401
3.2 Cobalt based magnetic nanoparticles 402
3.3 Iron based magnetic particles 402
3.4 Encapsulated magnetic nanoparticles 403
3.5 Biocompatibility issues of magnetic nanoparticles 403
Contents xxiii
4 Application of Magnetic Nanoparticles as Drug Carriers 404
4.1 Magnetic hyperthermia 405
4.2 Magnetic chemotherapy 406
4.3 Other magnetic treatment approaches 408
4.4 Magnetic gene transfer 409
5 Conclusions 410
References 411
19. DQAsomes as Mitochondria Specific Drug and DNA Carriers 419
Volkmar Weissig
1 Introduction 419
2 The Self Assembly Behavior of Bis Quinolinium Derivatives 420
2.1 Monte Carlo computer simulations 420
2.2 Physico chemical characterization 421
2.3 Structure activity relationship studies 422
3 DQAsomes as Mitochondrial Transfection Vector 424
4 DQAsomes as Carriers of Pro apoptotic Drugs 429
5 Summary 432
References 432
20. Liposomal Drug Carriers in Cancer Therapy 437
Alberto A. Gabizon
1 Introduction 437
2 The Challenge of Cancer Therapy 439
3 The Rationale for the Use of Liposomal Drug Carriers in Cancer . . 442
4 Liposome Formulation and Pharmacokinetics — Stealth
Liposomes 445
5 Preclinical Observations with Liposomal Drug Carriers
in Tumor Models 448
6 Liposomal Anthracyclines in the Clinic 449
6.1 Doxil 450
6.2 Myocet 454
6.3 Daunoxome 454
7 Clinical Development of Other Liposome entrapped
Cytotoxic Agents 455
8 The Future of Liposomal Nanocarriers 456
References 457
xxiv Contents
21. Nanoparticulate Drug Delivery to the Reticuloendothelial System
and to Associated Disorders 463
Mukul Kumar Basu and Sanchaita Lala
1 Introduction 463
2 Reticuloendothelial System and Associated Disorders 464
3 Uptake of Nanoparticles by the Reticuloendothelial System 464
3.1 Sites of uptake 464
3.2 Mechanism of uptake 465
3.3 Factors influencing uptake 468
3.4 Role of surface modifications on uptake 469
4 Active Targeting of Nanoparticles by Receptor Mediated
Endocytosis 471
5 Application in Chemotherapy 473
6 Summary 475
References 477
22. Delivery of Nanoparticles to the Cardiovascular System 481
Ban An Khazv
1 Introduction 481
2 Targeting the Myocardium with Immunoliposomes 481
3 Other Nanoparticle Targeting of the Cardiovascular System 484
4 Novel Application of Nano Immunoliposomes 485
5 CSIL as Targeted Gene or Drug Delivery 492
6 Conclusion 495
References 496
23. Nanocarriers for the Vascular Delivery of Drugs to the Lungs 499
Thomas Dziubla and Vladimir Muzykantov
1 Introduction 500
2 Biomedical Aspects of Drug Delivery to Pulmonary Vasculature . . 500
2.1 Routes for pulmonary drug delivery: Intratracheal vs
vascular 501
2.2 Pulmonary vasculature as a target for drug delivery 501
3 Pulmonary Targeting of Nanocarriers 503
3.1 Effects of carrier size on circulation and tissue distribution . . 503
Contents xxv
3.2 Passive targeting 505
3.2.1 Mechanical retention 505
3.2.2 Charge mediated retention and non viral gene
delivery 506
3.2.3 Pulmonary enhanced permeation retention (EPR)
effect 507
3.3 Active targeting 507
4 Carrier Design 509
4.1 Biocompatibility 509
4.2 Material selection (by application) 510
4.2.1 Imaging 510
4.2.2 Gene delivery 510
4.2.3 Delivery of therapeutic enzymes 511
4.2.4 Small molecule drugs 512
4.3 Types of nanocarriers 512
4.4 Mechanisms of drug loading 512
4.5 Drug release mechanisms 515
4.6 Nanocarriers for active targeting 516
5 Conclusion: Safety Issues, Limitations and Perspectives 517
References 518
24. Nanoparticulate Carriers for Drug Delivery to the Brain 527
Jorg Kreuter
1 Introduction 527
2 Nanoparticles 528
3 Biodistribution 530
3.1 Influence of surfactants on the biodistribution of
nanoparticles 530
3.2 Influence of PEGylation on the biodistribution of
nanoparticles 532
4 Pharmacology 534
5 Brain Tumors 536
6 Toxicology 538
7 Mechanism of the Delivery of Drug Across the Blood Brain
Barrier with Nanoparticles 539
8 Summary 541
9 Conclusions 542
References 542
xxvi Contents
25. Nanoparticles for Targeting Lymphatics 549
William Phillips
1 Introduction 549
1.1 The lymphatic vessels 550
1.2 Lymph nodes 551
2 Potential for Nanoparticles for Drug Delivery to Lymphatics . 553
3 Importance of Lymph Nodes for Disease Spread and
Potential Applications of Lymph Node Drug Delivery 554
3.1 Cancer 554
3.2 HIV 555
3.3 Filaria 555
3.4 Anthrax 556
3.5 Tuberculosis 556
3.6 Importance of lymph node antigen delivery for development
of an immune response 557
4 Factors Influencing Nanoparticle Delivery to Lymph Nodes 559
4.1 Nanoparticle size 559
4.2 Nanoparticle surface 559
4.3 Effect of massage on lymphatic clearance of subcutaneously
injected liposomes 560
4.4 Macrophage phagocytosis 561
4.5 Fate of nanoparticles in lymph nodes 561
5 Nanoparticle Diagnostic Imaging Agents for Determining Cancer
Status of Lymph Nodes 561
5.1 Subcutaneous injection of iodinated nanoparticles for
computed tomography imaging 561
5.2 Subcutaneous and intraorgan injection of magnetic
resonance (MRI) contrast agents 563
5.3 Intravenous injection of magnetic nanoparticles for
MRI imaging 563
5.4 Nanoparticle diagnostic agents for localizing the sentinel
lymph node 565
5.5 Radiolabeled nanoparticles for sentinel lymph node
identification 566
5.6 "mTc Colloidal nanoparticles for sentinel node identification . 566
5.7 Optical 568
5.8 Ultrasound nanobubbles 569
6 Recently Introduced Medical Imaging Devices for Monitoring
Lymph Node Delivery and Therapeutic Response 569
Contents xxvii
7 Nanoparticle Lymph Node Drug Delivery 571
7.1 Confusion in reporting lymph node delivery 571
7.2 Calculation of lymph node retention efficiency 573
8 Specific Types Nanoparticles for Lymph Node Targeting 573
8.1 PLGA nanoparticles 573
8.2 Micelles 574
8.3 Liposomes 574
9 Avidin Biotin Liposome Lymph Node Targeting Method 577
10 Massage and the Avidin Biotin Liposome Targeting Method 578
11 Nanoparticles for Lymph Node Anti Infectious Agent Delivery . . . 580
12 Liposomes for Intraperitoneal Lymph Node Drug Delivery 581
12.1 Intraperitoneal liposome encapsulated drugs 582
12.2 Effect of liposome size on intraperitoneal clearance 583
12.3 Avidin/Biotin liposome system for intraperitoneal and
lymph node drug delivery 584
12.4 Mediastinal lymph node drug delivery with avidin biotin
system by intrapleural injection 585
12.5 Avidin biotin for diaphragm and mediastinal lymph node
targeting 586
13 Nanoparticles for Cancer Therapy 587
13.1 Intralymphatic drug delivery to lymph nodes 587
13.2 Nanoparticles for treatment of metastatic lymph nodes of
upper GI malignacies 589
13.3 Lessons from endolymphatic radioisotope therapy 591
14 Advantages of Nanoparticles for Lymphatic Radiotherapy 592
15 Intraoperative Radiotherapy for Positive Tumor Margins
and for Treatment of Lymph Nodes 593
16 Potential of Using Radiolabeled Nanoparticles for Intratumoral
Radionuclide Therapy 593
17 Liposome Pharmacokinetics after Intratumoral Administration . . .595
18 Rhenium Labeled Liposomes for Tumor Therapy 595
19 Nanoparticles for Immune Modulation 597
20 Conclusions 598
References 598
26. Polymeric Nanoparticles for Delivery in the Gastro Intestinal Tract 609
Mayank D. Bhavsar, Dinesh B. Shenoy and Mansoor M. Amiji
1 Oral Drug Delivery 609
xxviii Contents
2 Anatomical and Physiological Considerations of Gastro intestinal
Tract (GIT) for Delivery 610
3 Introduction to Polymeric Nanoparticles as Carriers 614
4 Preparation of Polymeric Nanoparticles 615
5 Design Consideration for Nanoparticle based Delivery Systems . . 619
5.1 Polymer characteristics 619
5.2 Drug characteristics 620
5.3 Application characteristics 621
6 Nanoparticles in Experimental and Clinical Medicine 621
6.1 Drug delivery in the oral cavity 621
6.2 Gastric mucosa as a target for oral nanoparticle mediated
therapy 625
6.3 Nanoparticles for delivery of drugs and vaccines in the small
intestine 626
6.4 Nanoparticles for colon specific delivery 632
7 Integrating Polymeric Nanoparticles and Dosage Forms 634
8 Toxicology and Regulatory Aspects 636
8.1 Safety 637
8.2 Quality of material/characterization 638
8.3 Environmental considerations 638
9 Conclusion and Outlook 639
References 640
27. Nanoparticular Carriers for Ocular Drug Delivery 649
Alejandro Sanchez and Maria f. Alonso
1 Biopharmaceutical Barriers in Ocular Drug Delivery. Classification
of Nanoparticulate Carriers for Ocular Drug Delivery 650
2 Nanoparticulate Polymer Compositions as Topical Ocular Drug
Delivery Systems 651
2.1 First generation: Polymer nanoparticles and nanocapsules
for topical ocular drug delivery 652
2.1.1 Acrylic polymers based nanoparticles 654
2.1.2 Polyester based nanoparticles and nanocapsules . . .655
2.1.3 Polysaccharide based nanoparticles 657
2.2 Second nanoparticles generation: The coating approach . 659
2.2.1 Polyacrylic coating 659
2.2.2 Polysaccharide coating 660
2.2.3 Polyethyleneglycol (PEG) coating 662
Contents xxix
2.3 Third nanoparticles generation: Towards functionalized
nanocarriers 663
3 Nanoparticulate Polymer Compositions as Subconjuctival Drug
Delivery Systems 665
4 Nanoparticulate Polymer Compositions as Intravitreal Drug
Delivery Systems 665
5 Conclusions and Outlook 667
References 668
28. Nanoparticles and Microparticles as Vaccine Adjuvants 675
Janet R. Wendorf, Manmohan Singh and Derek T. O'Hagan
1 Introduction 675
2 Nanoparticle and Microparticle Preparation Methods 678
2.1 Nanoparticles and microparticles made from polyesters . 678
2.2 Nanoparticles and microparticles made with chitosan 681
2.3 Other nanoparticles and microparticles 681
3 Adjuvant Effect of Nanoparticles and Microparticles 681
3.1 Nanoparticles and microparticles as mucosal adjuvants . 682
3.2 Nanoparticles and microparticles as systemic adjuvants . 686
4 Delivery of DNA Using Nanoparticles and Microparticles 688
5 Conclusions 690
References 691
29. Pharmaceutical Nanocarriers in Treatment and Imaging of Infection 697
Raymond M. Schiffelers, Gert Storm and Irma A. ]. M. Bakker Woudenberg
1 Introduction 697
2 Carriers that are Easily Recognized as Foreign Materials 698
3 Carriers that Avoid Recognition as Foreign Materials 701
4 Local Application of Carriers 705
5 Concluding Remarks 706
References 707
Index 713 |
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any_adam_object_boolean | 1 |
author_GND | (DE-588)112659381 |
building | Verbundindex |
bvnumber | BV021629143 |
callnumber-first | R - Medicine |
callnumber-label | RS201 |
callnumber-raw | RS201.N35 |
callnumber-search | RS201.N35 |
callnumber-sort | RS 3201 N35 |
callnumber-subject | RS - Pharmacy |
classification_rvk | VX 8560 |
ctrlnum | (OCoLC)255837779 (DE-599)BVBBV021629143 |
dewey-full | 615.6 |
dewey-hundreds | 600 - Technology (Applied sciences) |
dewey-ones | 615 - Pharmacology and therapeutics |
dewey-raw | 615.6 |
dewey-search | 615.6 |
dewey-sort | 3615.6 |
dewey-tens | 610 - Medicine and health |
discipline | Chemie / Pharmazie Medizin |
discipline_str_mv | Chemie / Pharmazie Medizin |
format | Book |
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oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-014844071 |
oclc_num | 255837779 |
open_access_boolean | |
owner | DE-29 DE-19 DE-BY-UBM DE-20 |
owner_facet | DE-29 DE-19 DE-BY-UBM DE-20 |
physical | XXIX, 724 S. Ill., graph. Darst. |
publishDate | 2006 |
publishDateSearch | 2006 |
publishDateSort | 2006 |
publisher | Imperial College Press |
record_format | marc |
spelling | Nanoparticulates as drug carriers ed. Vladimir P. Torchilin London Imperial College Press 2006 XXIX, 724 S. Ill., graph. Darst. txt rdacontent n rdamedia nc rdacarrier Biomedical materials Nanoparticles Nanostructured materials Arzneistoffträger (DE-588)4278196-6 gnd rswk-swf Nanopartikel (DE-588)4333369-2 gnd rswk-swf Nanokapsel (DE-588)4330956-2 gnd rswk-swf Nanopartikel (DE-588)4333369-2 s Arzneistoffträger (DE-588)4278196-6 s Nanokapsel (DE-588)4330956-2 s DE-604 Torčilin, Vladimir P. 1946- Sonstige (DE-588)112659381 oth HBZ Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=014844071&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
spellingShingle | Nanoparticulates as drug carriers Biomedical materials Nanoparticles Nanostructured materials Arzneistoffträger (DE-588)4278196-6 gnd Nanopartikel (DE-588)4333369-2 gnd Nanokapsel (DE-588)4330956-2 gnd |
subject_GND | (DE-588)4278196-6 (DE-588)4333369-2 (DE-588)4330956-2 |
title | Nanoparticulates as drug carriers |
title_auth | Nanoparticulates as drug carriers |
title_exact_search | Nanoparticulates as drug carriers |
title_exact_search_txtP | Nanoparticulates as drug carriers |
title_full | Nanoparticulates as drug carriers ed. Vladimir P. Torchilin |
title_fullStr | Nanoparticulates as drug carriers ed. Vladimir P. Torchilin |
title_full_unstemmed | Nanoparticulates as drug carriers ed. Vladimir P. Torchilin |
title_short | Nanoparticulates as drug carriers |
title_sort | nanoparticulates as drug carriers |
topic | Biomedical materials Nanoparticles Nanostructured materials Arzneistoffträger (DE-588)4278196-6 gnd Nanopartikel (DE-588)4333369-2 gnd Nanokapsel (DE-588)4330956-2 gnd |
topic_facet | Biomedical materials Nanoparticles Nanostructured materials Arzneistoffträger Nanopartikel Nanokapsel |
url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=014844071&sequence=000002&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
work_keys_str_mv | AT torcilinvladimirp nanoparticulatesasdrugcarriers |