Microdialysis (MD) is an innovative clinical technique for measuring inters
titial tissue pharmacokinetics and plasma-to-tissue transfer rates of drugs
in humans. However, microdialysis requires the availability of specialized
analytical techniques. Capillary electrophoresis (CE), which enables conce
ntration measurements of small volume samples, theoretically constitutes an
ideal analytical technique for measuring drug concentrations in microdialy
sates. In the present experiments, we aimed at assessing the potential util
ity and limitations of CE for analysis of microdialysates in a clinical sit
uation. Microdialysates were obtained from primary breast cancer patients w
ho received chemotherapy including 5-fluorouracil (5-FU; 600 mg/m(2)). Subs
equently, 5-FU concentrations were measured in tumor - and subcutaneous adi
pose tissue - microdialysates by CE. By combining MD and CE, complete time
versus concentrations profiles could be obtained for 5-FU in the interstiti
al tumor space and important clinical questions could be addressed. We conc
lude that the combination of MD and CE leads to important anti previously i
naccessible information about the drug distribution process in a clinical s
etting.