The microdialysis technique has undergone much development since its first use in 1972, when it was first employed to monitor concentrations of endogenous biomolecules in the brain. Today's area of application has expanded to monitoring free concentrations of endogenous as well as exogenous compounds in virtually any tissue. Although microdialysis is still primarily used in preclinical animal studies (e.g. laboratory rodents, dogs, sheep, pigs), it is now increasingly employed in humans to monitor free, unbound drug tissue concentrations as well as interstitial concentrations of regulatory cytokines and metabolites in response to homeostatic perturbations such as feeding and/or exercise.
When employed in brain research, microdialysis is commonly used to measure neurotransmitters (e.g. dopamine, serotonin, norepinephrine, acetylcholine, glutamate, GABA) and their metabolites, as well as small neuromodulators (e.g. cAMP, cGMP, NO), amino acids (e.g. glycine, cysteine, tyrosine), and energy substrates (e.g. glucose, lactate, pyruvate). Exogenous drugs to be analyzed by microdialysis include new antidepressants, antipsychotics, as well as antibiotics and many other drugs that have their pharmacological effect site in the brain. The first non-metabolite to be analyzed by microdialysis in vivo in the human brain was rifampicin.
Applications in other organs include the skin (assessment of bioavailability and bioequivalence of topically applied dermatological drug products), and monitoring of glucose concentrations in patients with diabetes (intravascular or subcutaneous probe placement). The latter may even be incorporated into an artificial pancreas system for automated insulin administration.
Microdialysis has also found increasing application in environmental research, sampling a diversity of compounds from waste-water and soil solution, including saccharides, metal ions, micronutrients, organic acids, and low molecular weight nitrogen. Given the destructive nature of conventional soil sampling methods, microdialysis has potential to estimate fluxes of soil ions that better reflect an undisturbed soil environment.