We describe a fluorometric technique for the measurement of transport
parameters of fluorescent drugs through cellular membranes, Unlike oth
er procedures, this method gives an accurate measure of drug accumulat
ed in the cells and measures the fraction of free and bound drug in th
e cell. The kinetic parameters of transport through cellular membranes
are determined using a simple three-compartment model combined with f
luorescence measurements performed on the extracellular medium and on
Triton-permeabilized cells during daunorubicin incorporation, With thi
s technique we found that LoVo cells have a greater daunorubicin uptak
e, a similar input rate constant and a lower output rate constant than
the drug-resistant LoVo/DX cells.