Anders Buur and Niels M0rk

contents

9.1 Introduction 135

9.2 The Prodrug Principle 136

9.3 Design of Prodrugs—Chemical Considerations 137

9.3.1 Prodrugs Transformed by Enzymatic Reactions 137

9.3.2 Prodrugs Transformed by Spontaneous Reactions 138

9.4 Design of Prodrugs—Application of the Prodrug Principle 140

9.4.1 Design of Prodrugs with Improved Bioavailability 140

9.4.1.1 Improved Aqueous Solubility 141

9.4.1.2 Improved Biomembrane Permeability (Passive Diffusion) 141

9.4.1.3 Improved Transporter-Mediated Permeability 143

9.4.1.4 Increased Stability in the Gastrointestinal Tract 143

9.4.1.5 Improved Metabolic Stability 144

9.4.2 Design of Prodrugs for Prolonged Drug Action 146

9.4.2.1 Intramuscular Depot Injections 146

9.4.2.2 Macromolecular Prodrugs 146

9.4.3 Design of Produgs for Drug Targeting 146

9.5 Development of Prodrugs 148

9.5.1 Safety Assessment of Prodrugs 148

9.6 Concluding Remarks 148

Further Readings 149

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