A nonsteroidal anti-inflammatory drug, piroxicam, was administered from a c
ommercially available gel to human volunteers both passively and under the
application of an iontophoretic current. The effect of occlusion on the pas
sive delivery of piroxicam was also examined in a separate series of experi
ments. After treatment, the stratum corneum (SC) at the site of application
was progressively tape-stripped and piroxicam transport into the membrane
was assessed by UV analysis of drug extracted from the tape-strips. Analysi
s of variance did not show any significant difference between passive pirox
icam delivery after 30, 60 or 125 nun. However, current application enhance
d drug uptake into the SC, as indicated by both increased piroxicam concent
rations in the horny layer and detectable concentrations at greater depths
into the membrane. The total amount of drug recovered in the SC post-iontop
horesis was significantly higher than that found following passive diffusio
n for each application time. The amounts of drug recovered from the tapes a
fter 60 and 125 min of current application were significantly higher than t
hat after 30 min treatment. Finally, the in vivo SC concentration profiles
following passive delivery were fitted to the appropriate solution of Fick'
s second law of diffusion to determine skin partitioning and diffusivity pa
rameters. (C) 2001 Elsevier Science B.V. All rights reserved.