Introduction to the Microdialysis Technology -- Recovery and Calibration Techniques: Toward Quantitative Microdialysis -- Analytical Considerations for Microdialysis Sampling -- Regulatory Aspects of Microdialysis: A United States Food & Drug Administration Perspective -- Microdialysis in CNS PKPD Research: Unraveling Unbound Concentrations -- Microdialysis in Antibiotic Research -- Skin and Transdermal Drug Delivery: Advantages and Challenges -- Translational Approaches For Predicting CNS Drug Effects Using Microdialysis -- Extracellular Amyloid-β Protein Dynamics in Alzheimer's Disease -- Microdialysis in Pain Research -- Microdialysis in Ocular Drug Development -- Microdialysis in Metabolic Research -- High Molecular Weight Targets and Treatments Using Microdialysis -- Complementary Techniques – Positron Emission Tomography -- Open Flow Microperfusion: An Alternative Method to Microdialysis? -- Microdialysis in Internal Organs and Tumors.

In vivo target site concentrations are probably the most important determinant of drug effects. Traditionally, linking drug concentrations to drug effects has been accomplished by modelling blood-derived data, mostly because a direct quantification of tissue concentrations has been beyond technical reach. Today, a direct measurement of target site concentrations is possible by employing microdialysis or complementary approaches such as imaging technologies. Microdialysis, initially conceived in the 1970ies, has become a standard tool in drug development. This comprehensive overview of current microdialysis technology covers general and disease-specific aspects of microdialysis by international experts in the field. It provides useful information for colleagues in academia and industry who are interested PK-PD aspects of drug development.