Abstract

The evaluation of absorption and availability at the site of action of a drug candidate is an important element of drug discovery and development, as clinical response is a function of the bioavailability of the active agent and its continued presence at the site of action. Evaluation of dermal pharmacokinetics facilitates the selection of new compounds or chemical structures for advancement as possible clinical candidates. An advantage of microdialysis is that it allows the measurement of compound concentrations at the site of action without disturbing the tissue milieu, making it possible to determine the relationship between this important variable and plasma concentrations of the agent. Described in this unit are laboratory protocols for performing dermal microdialysis experiments in rat for the purpose of defining the pharmacokinetics parameters of test agents.

By Nivea M. F. Voelkner, Alexander Voelkner & Hartmut Derendorf