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Heterogeneity is an inherent character of cell populations [1].It has been demonstrated that the variability in daunorubicin accumulation (i.e.net uptake) in patients leukemia cells may be related to chemotherapy outcome [2].The heterogeneity in doxorubicin (DOX) uptake by human leukemia K562 cells was determined by single-cell analysis using capillary electrophoresis (CE) coupled with laser-induced fluorescence (LIF) detection following drug treatment in vitro depended on two dosage schedules.First, as the single-and-high dose schedules, K562 cells were treated with 0.3, 3, 30, and 60 μM DOX for 36 h each, respectively.Second, as the multidose schedules, K562 cells were treated with 0.1, 1, 10, and 20 μM DOX for 12 h each, respectively, consecutively treating three times.A marked heterogeneity in DOX uptake among single K562 cells was observed.This cellular heterogeneity in DOX uptake is much less for the single-and-high dose schedules than that for the multi dose schedules.MTT and flow cytometry profiles of various DOX-treated cell populations indicated that the less variation in drug uptake lead to higher cytotoxicity.These results suggest that the optimization of therapy schedules can reduce the difference in drug uptake by cancer cells, and eventually improve the chemotherapy outcome.