Drug Targeting Technology: Physical, Chemical and Biological Methods (Drugs and the Pharmaceutical Sciences: a Series of Textbooks and Monographs)

Drugs and the Pharmaceutical Sciences 115......Page 1
Drug Targeting Technology: Physical, Chemical and Biological Methods......Page 2
Preface......Page 4
Contents......Page 8
Contributors......Page 10
I. INTRODUCTION......Page 12
A. pH......Page 13
B. Ionic State......Page 14
D. Gastric Emptying......Page 15
F. Age......Page 16
B. Stability of Polymers......Page 17
1. Single/multiple Layer Coating......Page 18
2. Organic and Aqueous Coating......Page 21
1. Thickness......Page 22
3. Other Excipients......Page 23
1. Tablets......Page 25
3. Multiple Units......Page 26
A. In Vitro–In Vivo Correlation......Page 28
B. In Vivo Testing......Page 29
V. APPLICATIONS......Page 32
VI. OUTLOOK......Page 35
REFERENCES......Page 36
II. PHYSIOLOGICAL REALITIES AND COLONIC ABSORPTION......Page 41
III. GOALS OF COLON TARGETING......Page 42
A. Current Prolonged-Release Materials......Page 43
IV. PHYSIOLOGICAL REQUIREMENTS FOR COLON TARGETING......Page 45
V. TESTING COLONIC BIODEGRADATION......Page 46
2. Glycoside-Prodrugs......Page 48
4. Dextran Prodrugs......Page 49
2. Oligosaccharides and Polysaccharides......Page 50
4. Chitosan......Page 53
REFERENCES......Page 54
II. INTRODUCTION......Page 60
A. Pharmacodynamic Drug Characteristics......Page 62
C. Oral Bioavailability......Page 63
D. Delivery Systems, Deposition Ratio, and Regional Lung Deposition......Page 64
E. Pulmonary Residence Time......Page 65
1. Dissolution Rate......Page 66
F. Modulation of Pulmonary Selectivity by Sustained-release Drug Delivery Systems......Page 67
G. Biological Interaction Leading to Prolonged Pulmonary Residence Time......Page 69
H. Speci.c Uptake into Cells......Page 70
A. Liposomes......Page 71
B. Microspheres and Microparticles......Page 78
C. Coated Particles......Page 79
E. Pulmonary Epithelial Cell Targeting......Page 80
F. Pulmonary Macrophage Targeting......Page 81
REFERENCES......Page 83
I. INTRODUCTION......Page 93
II. LIPID DIGESTION AND ABSORPTION AND THE PREABSORPTIVE PHASE......Page 94
IV. LIPIDS AND BIOAVAILABILITY ENHANCEMENT......Page 96
A. Bioavailability Enhancement by Means of Physicochemical Mechanisms......Page 97
B. Bioavailability Enhancement by Means of Biochemical/Metabolic Mechanisms......Page 103
V. LIPIDS AND TARGETING TO THE INTESTINAL LYMPH......Page 109
VI. LIPIDS AND DRUG BINDING TO PLASMA LIPOPROTEINS......Page 115
A. The Impact of Lipid-induced Alterations in Drug–LP Binding Pro.les on Drug Pharmacokinetics......Page 124
B. The Impact of Lipid-induced Alterations in Drug–LP Binding Pro.les on Drug Pharmacodynamics......Page 125
REFERENCES......Page 127
I. INTRODUCTION......Page 139
A. Vesicles Affect Skin Penetration In Vitro......Page 141
B. Vesicles Affect Skin Penetration In Vivo......Page 146
C. Conclusions......Page 150
A. Introduction......Page 152
C. Amphiphilic Molecules as Penetration Enhancers......Page 154
REFERENCES......Page 161
I. INTRODUCTION......Page 170
II. PRINCIPLES OF RETROMETABOLIC DRUG DESIGN......Page 172
III. SOFT DRUGS......Page 173
A. Loteprednol Etabonate......Page 175
IV. CHEMICAL DELIVERY SYSTEMS......Page 179
A. Brain-targeting Chemical Delivery Systems......Page 180
B. Estradiol-CDS......Page 184
V. CONCLUSIONS......Page 186
REFERENCES......Page 187
I. INTRODUCTION......Page 195
II. THE LIVER......Page 196
A. Parenchymal Cells......Page 197
B. Kupffer Cells......Page 198
C. Endothelial Cells......Page 200
D. Hepatic Stellate Cells......Page 201
A. Liver Cirrhosis or Fibrosis......Page 205
B. Infectious Liver Diseases......Page 207
C. Liver Cancer......Page 209
IV. CELL-SPECIFIC CARRIER SYSTEMS......Page 210
V. CRITICAL ASPECTS OF CONJUGATES TARGETED TO THE LIVER......Page 212
VI. MODIFIED ALBUMINS......Page 214
A. Chemical Preparation of the Modi.ed Albumins......Page 217
1. In Vivo Studies......Page 219
2. In Vitro Studies......Page 221
C. Drug-Albumin Conjugates......Page 222
1. Liver Cirrhosis or Fibrosis......Page 223
2. Infectious Liver Diseases......Page 225
3. Liver Cancer......Page 226
4. Diagnostic Purposes......Page 227
VII. CONCLUSIONS......Page 228
REFERENCES......Page 229
I. INTRODUCTION......Page 247
III. DNA CONDENSATION AND LOADING......Page 248
IV. PLASMID DELIVERY WITH ARTIFICIAL VIRAL ENVELOPES......Page 250
V. CONCLUSIONS......Page 253
REFERENCES......Page 254
I. SUMMARY......Page 255
III. THE DEVELOPMENT OF HVJ LIPOSOMES......Page 256
B. Penetration of the Vector into Tissues......Page 258
A. AVE Liposome: A New Anionic HVJ Liposome......Page 259
B. Development of HVJ-cationic Liposomes......Page 260
C. Malignant Glioma......Page 263
REFERENCES......Page 264
I. INTRODUCTION......Page 267
A. Immunological Approaches for the Modi.cation of Adenoviral Tropism......Page 268
B. Genetic Approaches for Modi.cation of Adenoviral Tropism......Page 270
III. TRANSCRIPTIONAL TARGETING......Page 271
C. Tumor-selective Promoters......Page 272
D. Treatment-responsive Promoters......Page 274
F. Enhancing the Activity of Tissue-speci.c or Other Selective Promoters......Page 275
IV. TARGETING OF VIRAL REPLICATION TO TUMORS......Page 276
A. Targeting of Tumor-speci.c Dysfunctions in Cells Cycle Control or Apoptosis by Adenovirus Mutants......Page 277
REFERENCES......Page 278