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Ketoprofen Tissue Permeation in Swine Following Cathodic Iontophoresis

PC Panus, PhD, PT, is Assistant Professor, Department of Physical Therapy, College of Public and Allied Health, East Tennessee State University, Box 70624, Johnson City, TN 37614-0624 (USA) (panus{at}access.etsu.edu). Address all correspondence to Dr Panus
KE Ferslew, PhD, is Professor, Section of Toxicology, Department of Pharmacology, James H Quillen College of Medicine, East Tennessee State University
B Tober-Meyer, DVM, is Director, Division of Laboratory Animal Resources, James H Quillen College of Medicine, East Tennessee State University
RL Kao, PhD, is Professor, Department of Surgery, James H Quillen College of Medicine, East Tennessee State University

Background and Purpose. Pharmacokinetic assessment of drug tissue permeation following iontophoresis is limited. The depth of ketoprofen tissue permeation following cathodic iontophoresis (4 mA, 40 minutes) and the stereoselectivity of drug delivery were examined in this study. Subjects. Ketoprofen (750 mg) was iontophoresed onto one porcine medial thigh, with passive drug permeation conducted on the other thigh. Methods. Skin, subcutaneous fascia, and muscle biopsies from the drug delivery sites were harvested and stored separately, and the "R" and "S" ketoprofen enantiomers were determined. Results. Iontophoretic and passive applications yielded equivalent total ketoprofen concentrations in the skin and fascia. In contrast, multivariate analysis demonstrated that the ketoprofen concentration in the first centimeter of muscle following iontophoresis was greater than the drug concentration in the deeper underlying muscle layers and greater than that delivered to any muscle layer following passive delivery. No transcutaneous stereoselective delivery of ketoprofen was detected. Conclusion and Discussion. Compared with passive delivery, iontophoresis enhances nonstereoselective ketoprofen permeation into the fascia-muscle interface. With delivery to deeper tissue sites, however, there is no apparent enhancement over passive application.

Key Words: Cutaneous administration • In vivo • Iontophoresis • Ketoprofen • Nonsteroidal anti-inflammatory drug

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