Transdermal delivery of interferon alpha-2B using microporation and iontophoresis in hairless rats

Abstract

Purpose: To demonstrate transdermal delivery of interferon alpha-2b (IFNalpha2b) in hairless rats through aqueous microchannels (micropores) created in the skin and enhanced by iontophoresis.

Materials and methods: The Altea Therapeutics PassPort System was configured to form an array of micropores (2.0 cm(2); 72 micropores/cm(2)) on the rat abdomen. The transdermal patch (Iomed TransQ1-GS-hydrogel) was saturated with an IFNalpha2b solution (600 microg/ml) and applied for 4 h. Delivery was evaluated with and without cathodic iontophoresis (0.1 mA/cm(2)). Intravenous delivery (0.4 microg/100 g body weight) was performed to support pharmacokinetic calculations.

Results: IFNalpha2b was not delivered through intact skin by itself (passive delivery) or during iontophoresis. However, passive delivery through micropores was achieved in vivo in rats. A dose of 397 +/- 67 ng was delivered over 6 h, with steady state serum concentrations reaching a plateau at 1 h post-patch application. These levels dropped rapidly after patch removal, and returned to baseline within 2 h of patch removal. Iontophoresis-enhanced delivery through micropores resulted in a two-fold increase in the dose delivered (722 +/- 169 ng) in the hairless rat.

Conclusions: In vivo delivery of IFNalpha2b was demonstrated through micropores created in the outer layer of the skin. Iontophoresis enhanced delivery through microporated skin in hairless rats.