دانلود کتاب Dermal Absorption Models in Toxicology and Pharmacology

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Preface......Page 6
Editor......Page 8
Contributors......Page 10
Contents......Page 12
Introduction......Page 14
Epidermis......Page 16
Layers of the Epidermis-Keratinocytes......Page 18
Epidermal Nonkeratinocytes......Page 22
Epidermal-Dermal Junction (Basement Membrane)......Page 24
Hypodermis......Page 25
Hair......Page 26
Glands of the Skin......Page 28
Conclusion......Page 30
References......Page 31
Introduction......Page 34
Preparation of Skin......Page 35
Receptor Fluid......Page 36
Lipophilic Compounds: Artificial Reservoir Effect......Page 37
Metabolism......Page 38
References......Page 39
Introduction......Page 42
Surgical Preparation and Perfusion......Page 44
Assessment of Flap Viability and Development of Biomarkers for Toxicity Assessment......Page 46
Absorption Studies......Page 48
Dermatopharmacokinetic Studies......Page 50
Quantitative Structure-Activity Relationship (QSAR) IPPSF Models......Page 52
Percutaneous Absorption of Vasoactive Chemicals......Page 54
Conclusion......Page 55
References......Page 56
Introduction......Page 62
Animal Model Selection......Page 63
In Vivo Methods for Assessment of Dermal Absorption......Page 64
Mass Balance......Page 65
Note on the Use of Radioactivity in Biological Fluids......Page 69
Tape-Stripping......Page 70
Indirect Difference or Surface Disappearance Method......Page 71
Microdialysis......Page 72
Pharmacodynamic Responses......Page 74
Attenuated Total Reflectance-Fourier Transform Infrared Spectroscopy......Page 75
Transepidermal Water Loss......Page 76
Conclusion......Page 77
References......Page 78
A Novel System Coefficient Approach for Systematic Assessment of Dermal Absorption from Chemical Mixtures......Page 84
Introduction......Page 85
Method Development......Page 86
Minor or Trace Chemicals......Page 87
System Coefficients of Sufficient Similar Mixtures......Page 88
Determination of the Solute Descriptors......Page 89
Selection of the Probe Compounds......Page 90
System Coefficients of Epidermis......Page 91
System Coefficients of Skin......Page 92
System Coefficients......Page 93
Major Components of Chemical Mixtures......Page 95
Solvent Effects......Page 96
Sodium Lauryl Sulfate Effects on Polydimethylsiloxane Absorption of Chemical Mixtures......Page 97
Advantages of the System Coefficient Approach......Page 99
References......Page 100
Introduction......Page 102
Biologically Based Pharmacokinetic Models......Page 103
Biologically Based Pharmacodynamic Models......Page 112
Acknowledgments......Page 120
References......Page 121
The Prediction of Skin Permeability Using Quantitative Structure-Activity Relationship Methods......Page 126
Quantitative Structure-Activity Relationships......Page 127
The Activity or Property to Be Modeled......Page 128
Physicochemical Properties and Structural Descriptors of the Molecules......Page 129
A Statistical Technique to Form the Relationship between Structure and Activity......Page 130
The Flynn Data Set......Page 131
Mechanistic Interpretation of the Potts and Guy Model......Page 137
Other Modeling Approaches......Page 138
Expert Systems......Page 140
Data Modeling by Nonexperts......Page 142
Recommendations for the Use of Quantitative Structure-Activity Relationships to Predict Skin Permeability Coefficients......Page 143
References......Page 144
Introduction......Page 148
Dermal Risk Assessment......Page 150
Examples of the Use of In Vitro Skin Penetration Data in Dermal Risk Assessment......Page 156
Environmental Contaminants......Page 157
Sunscreen Agent: Octyl Salicylate......Page 160
Hair Dyes: 2-nitro-4-aminodiphenylamine and N-1-(2-Hydroxyethyl)-2- nitro-p-phenylenediamine......Page 162
Conclusion......Page 163
References......Page 164
Introduction......Page 172
Pesticide Exposure......Page 173
Prophylactic Agents and Other Medications......Page 175
Permethrin Absorption Following Single Chemical and Mixture Exposure......Page 176
DEET Absorption Following Single Chemical and Mixture Exposure......Page 181
Conclusion......Page 183
References......Page 185
Introduction......Page 190
Method......Page 191
Model Assumptions and Rationale......Page 196
Airflow Dependence......Page 197
Skin Site......Page 199
Ingredient Interactions......Page 200
Conclusion......Page 201
References......Page 202
Introduction......Page 204
Materials and Methods......Page 205
Theory......Page 207
Results and Discussion......Page 210
Acknowledgments......Page 222
References......Page 223
Assessing Efficacy of Penetration Enhancers......Page 226
Advantages and Limitations of Penetration Enhancers......Page 227
Diffraction Studies......Page 228
Spectroscopic Studies......Page 230
Thermal Analysis......Page 233
Microscopic Studies......Page 234
Other Techniques......Page 235
Fatty Acids......Page 236
In Vivo Efficacy and Toxicity......Page 237
In Vitro Efficacy of Terpenes......Page 239
Azone......Page 245
In Vivo Efficacy and Toxicity......Page 246
Miscellaneous......Page 248
Conclusion......Page 250
References......Page 251
Dermal Blood Flow, Lymphatics, and Binding as Determinants of Topical Absorption, Clearance, and Distribution......Page 264
Principles of Dermal Clearance and Percutaneous Absorption......Page 265
Skin Microcirculation: Structure and Function......Page 267
Early Evidence of Changes in Topical Drug Absorption Caused by Altered Perfusion......Page 269
Isolated Perfused Tissue Models......Page 270
In Vivo Models......Page 271
Blood Flow......Page 272
Blood Flow and Tissue Distribution Kinetics......Page 274
Direct Deeper Tissue Penetration......Page 276
Effects of Vasoactive Drugs on Transdermal Penetration......Page 284
Clearance by Lymphatic Flow......Page 286
Pathological Conditions that Affect Cutaneous Blood Flow and Clearance......Page 288
References......Page 289
Introduction......Page 296
Mechanisms of Interactions......Page 299
Examples of Dermal Mixture Interactions......Page 300
Mixture Interactions Across Model Systems......Page 302
Can a Partition Coefficient Predict Mixture Behavior?......Page 305
Modified Quantitative Structure-Permeability Relationship Equations That Predict Chemical Absorption from a Mixture......Page 307
Potential Impact of Multiple Interactions......Page 311
References......Page 313
Introduction......Page 318
Theory......Page 320
Database Collection and Validation......Page 322
Inspection of the Data......Page 324
Regressions of the Validated Data to Structure-Activity Parameters......Page 331
Comparing Compounds Common to the Animal and Human Databases......Page 334
Conclusion......Page 340
References......Page 341
Appendix A: Permeability Coefficients and Input Parameters......Page 348
Appendix B: Documentation of Permeability Coefficient Data......Page 366
Appendix C: Review of Prior Comparisons of Animal Skin Permeability Coefficient Data (in Chronological Order)......Page 376
D......Page 382
I......Page 383
P......Page 384
R......Page 385
T......Page 386
X......Page 387