Journal
JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 99, Issue 2, Pages 712-718Publisher
ELSEVIER SCIENCE INC
DOI: 10.1002/jps.21856
Keywords
absorption; formulation vehicle; membrane transport; passive diffusion; skin; transdermal drug delivery
Funding
- Pfizer Global Research and Development, Ann Arbor, MI
- National Health and Medical Research Council of Australia
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We examined uptake of the model therapeutic agent, minoxidil, into appendages, stratum corneum (SC), and through human skin, under the influence of different vehicles. Quantitative estimation of therapeutic drug deposition into all three areas has not previously been reported. Finite doses of minoxidil (2%, w/v) in formulations containing varying amounts of ethanol, propylene glycol (PG), and water (60:20:20, 80:20:0, and 0:80:20 by volume, respectively) were used. Minoxidil in SC (by tape stripping), appendages (by cyanoacrylate casting), and receptor fluid was determined by liquid scintillation counting. At early times (30 min, 2 h), ethanol-containing formulations (60:20:20 and 80:20:0) caused significantly greater minoxidil retention in SIC and appendages, compared to the formulation lacking ethanol (0:80:20). A significant increase in minoxidil receptor penetration occurred with the PG-rich 0:80:20 formulation after 12 h. We showed that deposition of minoxidil into appendages, SC, and skin penetration into receptor fluid were similar in magnitude. Transport by the appendageal route is likely to be a key determinant of hair growth promotion by minoxidil. (C) 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 99:712-718, 2010
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