Abstract
Transdermal permeation of lornoxicam, one of potent non-steroidal anti-inflammatory drugs, was studied in vitro with various vehicles and fatty acids using hairless mouse dorsal skin and human cadaver full skin. Vehicles used were diethylene glycol monoethyl ether (DGME), propylene glycol monocaprylate, propylene glycol, oleyl alcohol, dimethyl sulfoxide (DMSO) and others. Various fatty acids were employed as enhancers. Among pure vehicles studied, only DMSO showed permeation from saturated solutions. In the case of DMSO–DGME co-solvent, the higher the DGME ratios were, the lower the fluxes were. The addition of fatty acid (3 w/v %) increased the permeation in the rank order of linoleic acid (LOA) ≥ oleic acid ≥ lauric acid > capric acid > caprylic acid. Enhancement ratios ranged from 2 to 37 compared to the flux without fatty acid. Lornoxicam flux decreased in inverse proportion to the concentration of triethanolamine (TEA), which was used as a salt former and solubilizer. However, the flux increased linearly as the donor dose increased even in the presence of TEA. Using human cadaver skin, the permeability of lornoxicam was much lower than that using the hairless mouse skin, but fluxes increased as the concentration of LOA increased. These results indicate the feasibility of lornoxicam transdermal delivery with a combination of fatty acid and TEA in DMSO or DMSO–DGME cosolvents.
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