Microencapsulation: Methods and Industrial Applications, 2nd edition (Drugs and the Pharmaceutical Sciences)

Front cover......Page 1
Preface to the Second Edition......Page 12
Preface to the First Edition......Page 14
Contents......Page 18
Contributors......Page 24
INTRODUCTION......Page 28
TECHNIQUES USING ORGANIC SOLVENTS Emulsification–Solvent Removal Processes......Page 29
Organic Phase Separation (Coacervation)......Page 32
Spray Drying......Page 34
TECHNIQUES WITHOUT ORGANIC SOLVENTS Residual Solvent Considerations......Page 35
Techniques Using Supercritical Fluids (SF)......Page 36
Dry Processes......Page 66
REFERENCES......Page 68
INTRODUCTION Categories of Pesticide Formulations......Page 81
Release Patterns from Encapsulated Formulations......Page 82
STANDARD MICROENCAPSULATION PROCESSES FOR PESTICIDES General Methods of Encapsulation......Page 85
Interfacial Polymerization......Page 86
Phase Separation......Page 90
Insect Growth Regulators (IGR)......Page 93
Essential Oils as Natural Pesticides......Page 94
Water-Soluble Pesticides......Page 96
Release Rate of Pesticide......Page 97
Acute Oral Toxicity to Mice......Page 98
Efficacy......Page 99
SUMMARY......Page 101
REFERENCES......Page 102
INTRODUCTION......Page 105
PULSATILE SYSTEMS......Page 109
pH-Controlled Systems......Page 110
Enzymatically Controlled Systems......Page 111
Systems with Rupturable Coatings......Page 112
Eroding Systems......Page 113
Rupturing Systems......Page 114
REFERENCES......Page 120
INTRODUCTION......Page 125
BIODEGRADABLE POLYMERS Introduction......Page 126
Poly(ester)s......Page 127
Poly(anhydride)s......Page 128
PHASE SEPARATION AND COACERVATION Introduction......Page 129
Application in Pharmacy......Page 131
W/O/W-DOUBLE EMULSION TECHNIQUE......Page 132
Principles of the Spray Drying Process......Page 139
Pharmaceutical Applications for Parenteral Depot Systems......Page 142
Pharmaceutical Products......Page 143
REFERENCES......Page 144
INTRODUCTION......Page 149
Covalent Binding of Ligand to the Liposomal Surface......Page 150
Noncovalent Methods Used to Bind Ligands to the Liposomal Surface......Page 160
Immunoliposomes and Active Targeting......Page 163
LABELING POLYMERIC NANOPARTICLES WITH LIGANDS......Page 164
Covalent and Multistep Approaches Used to Bind Ligands to the Surface of Nanoparticles......Page 165
HOW TO CHOOSE THE COUPLING METHOD......Page 167
REFERENCES......Page 168
INTRODUCTION......Page 175
Emulsification Process in Stirred Reactor......Page 178
Droplet Size Distribution......Page 185
Principles of Similarity......Page 190
Dynamic Similarity......Page 191
APPLICATIONS—EXAMPLES Example 1: Microencapsulation by Interfacial Polycondensation......Page 193
Example 2: Nanoencapsulation by Emulsification Diffusion......Page 199
NOTATIONS......Page 204
REFERENCES......Page 205
MEASUREMENT OF DRUG RELEASE......Page 209
Dialysis Bag Diffusion Techniques......Page 210
Continuous-Flow Methods......Page 211
MECHANISMS OF DRUG RELEASE......Page 212
DRUG RELEASE KINETIC MODELS Fick’s Law of Diffusion......Page 214
Release from Particulates......Page 215
Release from Microcapsules......Page 222
Regulated Drug Release......Page 223
EMPIRICAL MODELS AND COMPARISON OF DRUG RELEASE PROFILES......Page 224
Model-Independent Methods......Page 225
Model-Dependent Methods......Page 227
IN VITRO–IN VIVO CORRELATION......Page 229
SUMMARY......Page 230
REFERENCES......Page 231
INTRODUCTION: THE RATIONALE OF USING BIODEGRADABLE, NANOPARTICULATE SOLID LIPIDS IN DRUG DELIVERY......Page 239
Melt Homogenization......Page 242
Cold Homogenization......Page 249
Precipitation from Solvent-in-Water Emulsions......Page 250
Precipitation from O/W Microemulsions......Page 251
Precipitation from Organic Solution......Page 255
Particle Size and Size Distribution......Page 256
Morphology and Microstructure......Page 258
Surface Properties......Page 262
Drug Incorporation and Release......Page 263
Safety and Tolerability Aspects......Page 268
Systemic Administration......Page 271
Immunization and DNA Delivery......Page 277
Local Administration......Page 279
CONCLUSIONS......Page 281
REFERENCES......Page 283
INTRODUCTION......Page 295
Classical Cyclodextrins......Page 296
Amphiphilic Cyclodextrins......Page 299
Nanoparticle Preparation Methods......Page 304
Parameters Influencing Amphiphilic Cyclodextrin Nanoparticle Characteristics......Page 306
Nanocapsules......Page 308
Nanospheres......Page 309
REFERENCES......Page 317
INTRODUCTION......Page 323
PREPARATION OF LIPOSPHERES......Page 324
PHYSICAL CHARACTERIZATION OF LIPOSPHERES Structure......Page 325
Particle Size......Page 326
Drug Distribution......Page 327
APPLICATIONS OF LIPOSPHERES......Page 328
Parenteral Delivery of Local Anesthetics......Page 329
Parenteral Delivery of Antibiotics......Page 331
Parenteral Delivery of Vaccines and Adjuvants......Page 332
PLA Lipospheres for the Delivery of LHRH Analogs......Page 334
Topical Delivery of Insect Repellent......Page 336
Nanolipospheres for Cell Targeting of Anticancer Drugs......Page 338
In Situ Formation of Lipospheres for Oral Delivery of Cyclosporin......Page 339
SUMMARY......Page 340
REFERENCES......Page 341
INTRODUCTION......Page 343
LIPOSOMES: DEFINITION, NEEDS FOR, AND OUTLINE OF THEIR ADVANTAGES AND DRAWBACKS Liposomes: A Family of Structurally Related Microparticles......Page 344
Deficiencies in Treatment with Free Drugs that Justify the Pursuit of DDS and Consideration of Liposomes for the Task......Page 346
SELECTION OF THE LIPOSOME TYPE/SPECIES: VIEWS AND CRITERIA FROM ACADEMIC AND INDUSTRIAL RESEARCH AND THEIR PROPOSED INTEGRATION Liposome Type, Size, and Production Issues......Page 349
Lipid Composition......Page 351
Targeting: Definition, Stages, and Status......Page 352
The Means Through which Liposome Targeting has been Attempted and the Feasibility of Developing Liposomes as Pharmaceutical Products......Page 353
LIPOSOMES AS A STERILE, PYROGEN-FREE SYSTEM WITH PHARMACEUTICALLY ACCEPTABLE SHELF-LIFE, STABILITY, AND DOSAGE FORMS Sterile, Pyrogen-Free Liposomes......Page 356
Shelf-Life, Stability, and Dosage Forms......Page 357
LIPOSOME CHARACTERISTICS (PERCENTAGE OF ENCAPSULATION, KINETICS OF RELEASE, BIOLOGICAL ACTIVITY)—IN BASIC RESEARCH AND IN QUALITY ASSURANCE......Page 359
Efficiency of Drug Encapsulation......Page 360
Kinetics of Drug Release......Page 361
Biological Activities of Liposome-Encapsulated Drugs......Page 364
REFERENCES......Page 366
THE RATIONALE......Page 371
MICROEMULSIONS AS NANOVEHICLES......Page 374
PART I—MICROEMULSION PREPARATION AND MICROSTRUCTURES Drug Administration Routes......Page 375
Definitions and Concepts......Page 376
Microemulsions Composition and Ingredients......Page 380
Preparation......Page 382
Isotropic Regions and Phase Transitions......Page 386
Solubilization Capacities......Page 394
Modeling Compositions of Ingredients to Form ME......Page 395
Microemulsion Characterizations......Page 398
Small-Angle Scattering......Page 399
Other Methods......Page 410
PART II—POTENTIAL APPLICATIONS......Page 411
Oral Applications......Page 414
IV Microemulsions......Page 417
Skin Applications......Page 421
Ophthalmic Drugs......Page 436
Thermosetting Emulsions......Page 437
Delivery of Nutraceuticals......Page 438
FINAL REMARKS......Page 440
REFERENCES......Page 442
DEFINITION......Page 455
DRUG DELIVERY ISSUES......Page 456
Approaches for Improved Oral Delivery of Lipophilic Drugs......Page 457
Candidate Compounds for Oral Lipid-Based Formulations......Page 458
Oils......Page 459
Surfactants......Page 464
Cosolvents......Page 466
Ternary Diagrams......Page 467
Solubilization Properties......Page 469
Mechanism of Self-Emulsification......Page 470
Size......Page 472
Zeta Potential......Page 473
BIOPHARMACEUTICAL ASPECTS......Page 474
Effect of Surfactants......Page 475
Effect of Lipids......Page 478
Digestibility......Page 479
Dispersion......Page 481
The Lymphatic Pathway Opportunity......Page 482
Absorption Barriers......Page 490
THE STORY OF ORAL CYCLOSPORIN A......Page 492
THE ORAL PACLITAXEL CHALLENGE......Page 494
FUTURE AND PROSPECTS......Page 495
REFERENCES......Page 496
INTRODUCTION......Page 507
BLOOD AND MECHANISM OF ACTION OF HEPARINS......Page 508
ORAL DELIVERY OF HEPARINS......Page 509
Intestinal Absorption of Heparins Associated with Absorption Enhancers......Page 511
Polymeric Absorption Enhancers......Page 514
Drug Delivery Systems......Page 516
REFERENCES......Page 542
INTRODUCTION......Page 547
ABSORPTION OF POLYMERIC PARTICULATES FROM THE GI TRACT......Page 548
USE OF POLYMERIC PARTICLES FOR ORAL ADMINISTRATION......Page 553
Peptides and Proteins......Page 554
Other Active Drugs......Page 573
CONCLUSIONS......Page 578
REFERENCES......Page 579
DERMAL AND TRANSDERMAL DRUG DELIVERY......Page 589
The Nonviable Epidermis or SC......Page 590
The Viable Epidermis......Page 591
VESICLES AS SKIN DELIVERY SYSTEMS General......Page 592
The Effectiveness of Vesicles as Skin Drug Delivery Vehicles......Page 594
The Interactions of Vesicles with Animal and Human Skin......Page 596
The Effectiveness of Elastic Vesicles as Skin Delivery Vehicles......Page 598
The Interactions of Elastic Vesicles with Animal and Human Skin......Page 602
REFERENCES......Page 606
INTRODUCTION......Page 613
Glaucoma......Page 615
Dry Eye Syndrome or Keratoconjunctivitis Sicca......Page 616
Ocular Inflammation......Page 617
Ocular Infections......Page 618
LIPID AND POLYMERIC COLLOIDAL CARRIERS: DESCRIPTION AND CLASSIFICATION......Page 620
Anionic Emulsion......Page 622
Cationic Emulsion......Page 628
MICROEMULSIONS......Page 631
MULTIPLE EMULSIONS......Page 633
NANOPARTICLES Native Nanoparticles......Page 634
Surface Modified Nanoparticles......Page 639
NANOCAPSULES Native NCs......Page 640
Cationic Polymer-Coated NCs......Page 642
REFERENCES......Page 643
INTRODUCTION......Page 651
Interaction of Uncoated NP with Cultured Cells......Page 652
Interaction of Surface-Modified NP with Cultured Cells......Page 664
DISTRIBUTION AND PHARMACOKINETICS OF ANTICANCER DRUGS COUPLED TO NP......Page 665
Distribution of Anticancer Drugs Coupled to Nonmagnetic NP......Page 666
Distribution of Anticancer Drugs Coupled to Magnetic NP......Page 675
IN VIVO ACTIVITY AND TOXICITY OF ANTICANCER DRUGS COUPLED TO NP......Page 676
CONCLUDING REMARKS......Page 687
REFERENCES......Page 688
INTRODUCTION......Page 699
MICROSPHERE FORMULATION AND DEVELOPMENT Basic Formulation......Page 700
Pilot Production of Microspheres......Page 701
Understanding 5-FU Release Mechanisms......Page 703
Biocompatibility......Page 704
Efficacy Trials......Page 705
APPLICATION TO GLIOMA THERAPY AFTER TUMOR RESECTION: PHASE I–II AND IIB STUDIES......Page 708
STEREOTAXIC IMPLANTATION IN MALIGNANT GLIOMA: PHASE I STUDY......Page 710
CONCLUSION......Page 711
REFERENCES......Page 712
INTRODUCTION......Page 715
Dalargin......Page 716
Other Drugs......Page 719
Employment of Nanoparticles for the Therapy of Brain Tumors......Page 720
LONG CIRCULATING NANOPARTICLES FOR BRAIN DRUG DELIVERY......Page 723
MECHANISM OF NANOPARTICLE-MEDIATED DRUG TRANSPORT TO THE BRAIN......Page 725
CONCLUSIONS......Page 728
REFERENCES......Page 729
INTRODUCTION......Page 733
TYPES OF VESICULAR DELIVERY SYSTEMS Liposomes......Page 734
Nanoparticulate Systems......Page 736
Microemulsions......Page 737
Multiple Emulsions......Page 738
Liquid Crystals......Page 739
Solid Lipid Nanoparticles......Page 740
COMPOSITION Liposomes......Page 741
Nanoparticulate Systems......Page 742
Microemulsions......Page 743
Multiple Emulsions......Page 744
Solid Lipid Nanoparticles (SLNs)......Page 745
PRODUCTION Liposomes......Page 746
Nanoparticulate Systems......Page 748
Multiple Emulsions......Page 750
Liquid Crystals......Page 752
CHARACTERIZATION......Page 753
Microscopic Analyses......Page 754
Rheological Analysis......Page 755
Incorporation Efficiency Encapsulation of the Active Substances......Page 756
Microemulsions......Page 757
COSMETIC USES Liposomes......Page 758
Microemulsions......Page 761
Multiple Emulsions......Page 762
Solid Lipid Nanoparticle......Page 764
REFERENCES......Page 767
Index......Page 775
Back cover......Page 783