Abstract

Iontophoretic transport of penbutolol sulfate across porcine ear skin was studied. Passive transdermal flux of the drug in phosphate-buffered saline was 7.65 μg/cm2 hr. There was statistically significant flux enhancement when direct current iontophoresis was applied. Iontophoresis (0.11 mA/cm2, 0.17 mA/cm2, and 0.22 mA/cm2) for 6 hr, resulted in net transport of 87.36 μg/cm2, 137.51 μg/cm2, and 201.12 μg/cm2 of penbutolol sulfate, respectively. After 24 hr, cumulative amount of penbutolol transported were 201.63, 300.76, and 359.98 μg/cm2, respectively. There was a 2.20- (0.11 mA/cm2), 3.26- (0.17 m/Acm2), and 4.28-fold (0.22 mA/cm2) enhancement in transcutaneous steady-state flux values compared to passive delivery. Steady-state fluxes of penbutolol sulfate also increased proportionally to current density. Steady-state fluxes calculated from the linear portion of the cumulative amount versus time curves for penbutolol sulfate were 16.68, 24.97, and 32.76 μg/cm2/hr at current densities of 0.11, 0.17, and 0.22 mA/cm2. This study provides initial evidence for the potential use of iontophoresis for enhanced transdermal delivery of penbutolol sulfate.

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