Transdermal Drug Delivery Systems: Revised and Expanded

Transdermal Drug Delivery Second Edition, Revised and Expanded......Page 1
Drugs And The Pharmaceutical Sciences......Page 3
Additional Volumes In Preparation......Page 9
Preface......Page 10
Contents......Page 12
Contributors......Page 14
I. INTRODUCTION......Page 16
II. FICK’S LAWS OF DIFFUSION......Page 18
III. ESTIMATION OF PERMEABILITY COEFFICIENT FROM SIMPLE PHYSICOCHEMICAL PARAMETERS......Page 20
IV. DESIGN OF TRANSDERMAL DRUGS......Page 22
V. OTHER MODELING APPROACHES TO PREDICT FEASIBILITY OF DERMAL DELIVERY......Page 23
VI. ENHANCEMENT STRATEGIES......Page 24
VII. IN VITRO ASSESSMENTS......Page 27
VIII. IN VIVO ASSESSMENTS......Page 29
IX. TOXICITY......Page 31
REFERENCES......Page 32
II. BACKGROUND......Page 39
A. The Correlations......Page 40
B. The Flynn Database......Page 49
D. The Predictors log Kow and MW......Page 54
E. Reanalysis of the Flynn Database......Page 56
IV. CONCLUSIONS......Page 60
NOTATION......Page 61
APPENDIX......Page 62
REFERENCES......Page 66
I. INTRODUCTION......Page 70
II. DATA VALIDATION CRITERIA......Page 71
A. Adjustment for Ionization......Page 72
III. PERMEABILITY COEFFICIENT MODELS......Page 76
A. The Conventional Model......Page 78
B. Effect of Temperature......Page 79
C. Liquid Density (LD) Corrections and LD- Temperature Corrections......Page 80
D. The Two-Pathway Model......Page 82
E. Linear Solvation-Energy Relationships Model......Page 83
IV. RESULTS AND DISCUSSION......Page 84
A. Comparison with the Flynn Permeability Coef . cient Database......Page 86
B. Data Regression Analysis......Page 87
C. Analysis with the Conventional Model......Page 88
D. Trends in the FV Database......Page 89
F. Effect of Penetrant Liquid Density......Page 100
G. Analysis with the Two-Pathway Model......Page 106
H. Analysis with the LSER Model......Page 109
ACKNOWLEDGMENTS......Page 112
APPENDIX A. PERMEABILITY COEFFICIENTS AND INPUT PARAMETERS......Page 113
Anderson et al., 1988 (20)......Page 131
Blank, 1964 (58)......Page 132
Bronaugh and Congdon, 1984 (47)......Page 133
Dal Pozzo et al., 1991 (63)......Page 134
Hadgraft and Ridout, 1987 (37)......Page 135
Liu et al., 1994 (56)......Page 136
Morimoto et al., 1992 (25)......Page 137
Peck et al., 1995 (43)......Page 138
Roy and Flynn, 1989 (5)......Page 139
Roy and Flynn, 1990 (4)......Page 140
Roy et al., 1994 (38)......Page 141
Scheuplein and Blank, 1973 (53)......Page 142
Singh and Roberts, 1994 (45)......Page 143
APPENDIX C. LSER PARAMETERS......Page 144
GLOSSARY......Page 146
REFERENCES......Page 148
I. INTRODUCTION......Page 155
II. DATA VALIDATION CRITERIA......Page 156
A. Expression of the Stratum Corneum Concentration......Page 157
B. Effect of Ionization......Page 158
D. Equilibration Time......Page 159
B. Development of the Lipophilic – Hydrophilic Domain Model......Page 160
A. Examination of the Data......Page 162
B. Data Regression Analysis......Page 164
C. Analysis with the Conventional Model......Page 165
D. Trends in the Kcw Databases......Page 167
E. Analysis with the Lipophilic – Hydrophilic Domain Model......Page 177
F. Analysis with the LSER Model......Page 178
G. Estimation of the Stratum Corneum Diffusion Coef . cient......Page 180
H. Comparing the Database with Other Published Models......Page 181
I. Final Considerations and Recommendations......Page 184
V. CONCLUSIONS......Page 185
APPENDIX A. SC–WATER PARTITION COEFFICIENTS AND INPUT PARAMETERS......Page 186
Barry et al., 1985 (62)......Page 198
Hui et al., 1995 (25)......Page 199
Raykar et al., 1988 (3)......Page 200
Sato et al., 1991 (65)......Page 201
Surber et al., 1992 (21)......Page 202
Surber et al., 1990 (47)......Page 203
GLOSSARY......Page 204
REFERENCES......Page 206
INTRODUCTION......Page 211
A. A Basic Circuit of Iontophoresis......Page 212
B. Advantages and Limitations......Page 215
A. Electromigration......Page 216
B. The Convective Contribution: Electroosmosis......Page 220
C. Combined Electroosmosis and Electromigration Transport......Page 225
A. Peptides......Page 227
C. Analgesics......Page 228
E. Oligonucleotides......Page 229
F. Reverse Iontophoresis: A Noninvasive Tool for Clinical Sampling?......Page 230
REFERENCES......Page 231
I. INTRODUCTION......Page 238
A. Range of Compounds......Page 239
B. Magnitude and Onset Time of Enhancement......Page 240
C. In Vivo Studies......Page 242
III. MECHANISMS......Page 243
A. New Aqueous Pathways......Page 244
B. Thermal Effects......Page 245
D. Routes of Transport......Page 246
1. Pulse Waveform......Page 248
2. Pulse Voltage, Duration, Number and Rate......Page 250
B. Physicochemical Parameters of the Drug......Page 251
D. Modifying Agents......Page 252
A. Visual Evaluation......Page 253
B. In Vivo Noninvasive Investigation of the Skin......Page 254
C. Skin Electrical Properties......Page 255
E. Ultrastructure of the Skin......Page 256
A. Transdermal Drug Delivery......Page 257
B. Topical Drug Delivery......Page 258
REFERENCES......Page 259
I. INTRODUCTION......Page 266
II. THE PHYSICS OF ULTRASOUND PROPAGATION......Page 267
III. THE DESIGN OF PHONOPHORETIC SYSTEMS......Page 269
A. First-Order Forces......Page 270
B. Thermal Effects......Page 271
C. Radiation Pressure Force......Page 272
D. Microstreaming......Page 274
E. Cavitational Activity......Page 275
A. Steroids......Page 276
B. Indomethacin......Page 278
D. Other Drugs......Page 279
E. The Limitations of Animal Skin......Page 280
B. Steroids......Page 281
C. Proteins......Page 282
D. Other Drugs......Page 283
A. Nicotinate Esters......Page 285
C. Other Drugs......Page 286
VIII. ULTRASOUND FOR THE TRANSDERMAL EXTRACTION OF ANALYTES......Page 287
IX. CONCLUSIONS......Page 288
REFERENCES......Page 291
I. INTRODUCTION......Page 296
III. EPIDERMAL LIPID SYNTHESIS......Page 297
IV. STRUCTURAL BASIS FOR THE STRATUM CORNEUM BARRIER......Page 300
V. LAMELLAR BODY SECRETION......Page 301
VI. EXTRACELLULAR PROCESSING (ECP)......Page 302
VII. ORCHESTRATION OF EXTRACELLULAR PROCESSING BY THE STRATUM CORNEUM pH GRADIENT......Page 305
VIII. METABOLIC BASIS FOR ENHANCEMENT OF TRANSDERMAL DRUG DELIVERY......Page 306
IX. ASSESSMENT OF EFFICACY OF BIOCHEMICAL APPROACHES ( TABLE 4)......Page 310
REFERENCES......Page 312
I. INTRODUCTION......Page 316
III. PREPARATION OF SUPERSATURATED SOLUTIONS AND THEIR APPLICATION TO PERCUTANEOUS ABSORPTION......Page 319
A. Binary Mixtures......Page 320
B. Evaporation......Page 325
D. Reactions......Page 327
IV. APPLICATION OF SUPERSATURATION TO ACHIEVE SYNERGISTIC METHODS OF DRUG DELIVERY......Page 328
V. ANTINUCLEANT POLYMERS......Page 329
VI. CONCLUSIONS......Page 332
REFERENCES......Page 333
A. The Concept of Minimally Invasive Drug Delivery......Page 338
B. Mechanics of Skin Penetration......Page 340
1. Laser-Assisted Transdermal Delivery......Page 341
2. Direct Heat-Induced Microporation......Page 343
1. Tape-Stripping......Page 344
2. Suction Ablation......Page 345
3. Patch and Needle Arrays......Page 347
4. Skin Puncture Devices......Page 351
1. Overview of Fabrication Technology......Page 353
b. Single Hollow Microneedles......Page 354
c. Hollow Microneedle Arrays......Page 358
d. Solid Microneedle Arrays......Page 362
REFERENCES......Page 366
II. DRUG APPLICATIONS......Page 371
A. Regulatory Considerations for New Drug Applications ( NDA) as TDS......Page 372
B. Regulatory Considerations for Abbreviated New Drug Applications ( ANDA) as TDS......Page 373
IV. ENHANCER......Page 374
REFERENCES......Page 376