Percutaneous absorption-enhancing activity of urea derivatives.
The effect of urea and urea derivatives on the percutaneous absorption of salicylic acid and sodium salicylate through the skin of rabbit from petrolatum ointment was investigated. It was found that addition of urea or urea derivatives to the ointment base significantly increased the percutaneous absorption of the drugs in proportion to the concentration of the additive. The percutaneous absorption-enhancing activities of these compounds were that urea derivatives with the more and longer alkyl substituents showed the stronger activities. These activities of urea and urea derivatives were ascribed to the binding of these compounds with the lipids and proteins of the stratum corneum of the skin and the swelling of the tissues, which leads to the reduction of the barrier property of the layer. The preliminary skin irritation test showed that urea and urea derivatives were quite non-irritating to the skin. These results suggest that urea derivatives have a strong possibility to be developed as a percutaneous absorption enhancer.
D000818:Animals; D009824:Ointments; D011817:Rabbits; D020156:Salicylic Acid / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects*; D012980:Sodium Salicylate / Q000378:metabolism; D013268:Stimulation, Chemical; D014508:Urea / Q000031:analogs & derivatives* / Q000494:pharmacology* / Q000633:toxicity