Transdermal drug delivery (TDD) using electroporation is an attractive novel method of facilitated transport of compounds across skin that a short electrical pulse is applied to the skin, forcing the creation of a reversible transient aqueous pore to enhance drugs transdermal permeability. Most of prior researches are difficult to put into the practical use, such as stimulation for user and designing electroporater apparatus for TDD, due to pulse with high intensive. In this paper, the effect of electroporative energy on the transdermal fluxes of Tetracaini Hydrochlordum (TH) and Naproxenum is studied to explore a way of electroporative technique with low voltage. We applied a 120 V and 4.2 J square pulse to SD male rats skin on abdomen, the transdermal flux of TH increased 5.1 times more than the passive transport. While a 400 V and 37.6 J exponential decaying pulse was employed to same skin, the transdermal flux of Naproxenum was 3.5 times than passive transport. The results show that: (1) drugs transdermal permeably flux will create a saturation as the electroporative energy raises to threshold; (2) the transdermal energy efficiency (F/E value) declines as time extends; and (3) the effect of electroporation is concerned with the transdermal energy and drugs characteristics, electroporation is more effective than iontophoresis for TH, but conversely for Naproxenum. Transdermal drug delivery (TDD) using electroporation is an attractive novel method of facilitated transport of compounds across skin that a short electrical pulse is applied to the skin, forcing the creation of a reversible transient aqueous pore to enhance drugs transdermal permeability. Most of prior to researches are difficult to put into practical use, such as stimulation for user and designing electroporater apparatus for TDD, due to pulse with high intensive. In this paper, the effect of electroporative energy on the transdermal fluxes of Tetracaini Hydrochlordum (TH) and Naproxenum is studied to explore a way of electroporative technique with low voltage. We applied a 120 V and 4.2 J square pulse to SD male rats skin on abdomen, the transdermal flux of TH increased 5.1 times more than the passive transport. While a 400 V and 37.6 J exponential decaying pulse was employed to same skin, the transdermal flux of Naproxenum was 3.5 times than passive transport. The results sh ow that: (1) drugs transdermal permeably flux will create a saturation as the electroporative energy raises to threshold; (2) the transdermal energy efficiency (F / E value) declines as time extends; and (3) the effect of electroporation is concerned with the transdermal energy and drug  s characteristics, electroporation is more effective than iontophoresis for TH, but conversely for Naproxenum.