Regulatory authorities, such as the US Food and Drug Administration (FDA) and the Committee for Proprietary Medicinal Products (CPMP) of the European Union, have emphasized the value of human-tissue drug concentration data and support the use of clinical microdialysis to obtain this kind of pharmacokinetic information, showing the potential and significance of microdialysis. This book focuses on the use of microdialysis in drug evaluation for different organs and tissues and pharmacokinetics. The scope includes the introduction of basic principles, quantification and validation, analytical consideration, pharmacodynamic studies, pharmacokinetics, clinical aspects, and other applications of microdialysis. It provides a single reference source for microdialysis applied to the pharmaceutical area.