The objective was to optimize aminolevulinic acid (ALA) electrotransport into and through the skin by adjustment of formulation composition and ionic strength. ALA delivery was investigated as a function of the polarity and concentrations of drug and background electrolyte in the donor solution. The anodal iontophoretic flux of ALA from a 10% solution was compared with the drug's passive flux from the same formulation to which 5% dimenthyl sulphoxide (DMSO) had been added. Iontophoresis of the predominantly zwitterionic ALA from the anode is more efficient than that from the cathode. It was possible, though, to increase the electrotransport of ALA by simultaneously delivering the drug from both anode and cathode. Reduction of NaCl concentration in the anode led to a 3- to 4-fold increase in ALA flux. Transport of ALA across the skin and the amount of prodrug delivered into the skin (SC and [epidermis+dermis]) were ~4-fold greater with iontophoresis as compared to the passive application of the DMSO formulation. In conclusion: (a) electroosmosis from the anode is enhanced when the background electrolyte concentration is lowered; and (b) low-level iontophoresis enhances ALA transport across and, more importantly, into the [epiderms+dermis] than a simple formulation incorporating DMSO.