The Effect of Formulation Excipients on the Penetration and Lateral Diffusion of Ibuprofen on and within the Stratum Corneum Following Topical Application to Humans. Issue 3 (13th January 2014)

• Record Type: Journal Article
• Authors: Gee, Carol M.; Watkinson, Adam C.; Nicolazzo, Joseph A.; Finnin, Barrie C.
• Is Part Of: Journal of pharmaceutical sciences. Volume 103:Issue 3(2014:Mar.)
• Page Start: 909
• Page End: 919
• Publication Date: 2014-01-13
• Subjects: Pharmacy -- Periodicals; 615.1
• DOI: 10.1002/jps.23850
• Languages: English
• ISSNs: 0022-3549

Abstract

<abstract abstract-type="main" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Distribution profiles of topically applied drugs can be influenced by the presence of excipients. This study investigated the effect of common topical excipients on the simultaneous lateral diffusion and stratum corneum (SC) penetration of a model compound, ibuprofen (IBU) in humans. IBU solutions with and without propylene glycol (PG), polyethylene glycol 200 (PEG 200), and/or octisalate (OS) were dosed onto the forearm of participants. At various times, 10 "tape‐strippings" were obtained with perforated concentric tapes and analyzed for IBU concentration and SC protein mass. Complimentary <italic>in vitro</italic> permeation studies assessed the effect of excipients on the percutaneous absorption of IBU across human skin. Following <italic>in vivo</italic> application, IBU displayed a greater tendency for lateral diffusion when applied with OS, whereas IBU resisted lateral diffusion when dosed with PG and PEG 200. After 24 h, 25.3 ± 8.0% and 55.5 ± 18.6% of IBU was recovered from the SC <italic>in vivo</italic> with and without excipients, respectively. There was a twofold–to threefold enhancement in IBU flux <italic>in vitro</italic> when applied with excipients. The lower IBU recovery from the SC when applied with excipients may be attributed to the permeation enhancement effects of these excipients. The ability of IBU to laterally diffuse appears to be dependent on formulation excipients. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:909–919, 2014</p> </abstract>