The effect of different concentrations of drug and permeation enhancer (Dimethylsulfoxide) on iontophoretic transport of salbutamol sulphate was investigated in vitro. The iontophoretic transport was measured at constant (optimum) current density and pH as a function of varied concentration of drug, and at a fixed drug concentration as a function of permeation enhancer to know (i) how does drug concentration affect the efficiency of delivery? (ii) to what extent permeation enhancer affects the percutaneous delivery of drugs? (iii) what would be the combined effect of iontophoresis and permeation enhancer on permeation of drugs? Results showed that the use of different concentrations of drug in donor half cell (4, 8 and 16 mg/ml) increases the steady state flux both in passive diffusion (at pH 10.3) and iontophoresis (anodal at pH 7.4 and cathodal at pH 11) using 0.3 mA/cm2 current density. With the use of different concentrations of permeation enhancer (5, 10, 15 % w/v) in passive diffusion significantly increased (p < 0.05, t-test) the transport of drug and enhancement was 4, 6 and 7.6 folds respectively compared to the control. The maximum steady state flux was obtained with the use of 15 % w/v DMSO. Iontophoresis in conjugation with permeation enhancer had a significant synergistic effect in terms of transport of drug across skin