Transport Behavior of Hairless Mouse Skin During Constant Current DC Iontophoresis I: Baseline Studies

• Published in: Journal of pharmaceutical sciences 2011-04, Vol.100 (4), p.1475-1487
• Main Authors: Liddell, Mark R., Li, S. Kevin, Higuchi, William I.
• Format: Article
• Language: English
• Subjects: Administration, Cutaneous; Animals; Biological and medical sciences; Drug Delivery Systems - instrumentation; Equipment Design; Galvanic Skin Response; General pharmacology; Ions - administration & dosage; Ions - pharmacokinetics; iontophoresis; Iontophoresis - instrumentation; Male; Mannitol - administration & dosage; Mannitol - pharmacokinetics; Medical sciences; membrane conductance/resistance; Mice; Mice, Hairless; Permeability; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Raffinose - administration & dosage; Raffinose - pharmacokinetics; scintillation spectrometry; skin; Skin - metabolism; Skin Absorption; transdermal drug delivery; Urea - administration & dosage; Urea - pharmacokinetics
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.22381

The fluxes of charged and nonionic molecules across hairless mouse skin (HMS) were induced by direct current iontophoresis and used to characterize the transport pathways of the epidermal membrane. Experimental data were used to determine permeability coefficients from which the effective pore radii (Rp) of the transport pathways were calculated. Permeants used in these experiments were nonionic permeants (urea, mannitol, and raffinose), monovalent cationic permeants (sodium, tetraethylammonium, and tetraphenylphosphonium ions), and monovalent anionic permeants (chloride, salicylate, and taurocholate ions). The Rp estimates obtained by the anionic permeant pairs were 49, 22, and 20Å for the chloride/salicylate (Cl:SA), chloride/taurocholate (Cl:TC), and salicylate/taurocholate (SA:TC) pairs, respectively; with the cationic permeant pairs, the Rp values obtained were 19, 30, and 24Å for the sodium/tetraethylammonium (Na:TEA), sodium/tetraphenylphosphonium (Na:TPP), and the tetraethylammonium/tetraphenylphosphonium (TEA:TPP) pairs, respectively. Rp estimates for HMS obtained from nonionic permeant experiments ranged from 6.7 to 13.4Å. When plotted versus their respective diffusion coefficients, all of the permeability coefficients for the cationic permeants were greater than those of the anionic permeants. Additionally, the magnitudes of permeability coefficients determined in the current study with HMS were of the same order of magnitude as those previously determined in our laboratory using human epidermal membrane under similar iontophoresis conditions.