Percutaneous absorptoin-enhancing activity of urea derivatives
- 20 Downloads
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 concentratoin of the additive. The percutaneous absorptoin-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.
Key wordsPercutaneous absorption salicylic acid urea derivatives skin ointment
Unable to display preview. Download preview PDF.
- 1.Kydonieus, A.F. and Berner, B.:Trandermal Delivery of Drugs, Vol. I,II and III, CRC Press, Boca Raton, Florida (1987).Google Scholar
- 2.Chien, Y.W.:Transdermal Controlled Systemic Medications, Marcel Dekker, New York (1987).Google Scholar
- 3.Tyle, P.:Drug Delivery Devices, Marcel Dekker, New York, p. 385 (1988).Google Scholar
- 4.Katz, M. and Poulsen, B.J.:Handbook of Experimental Pharmacology, Vol. 28, pt.1, Springer Verlag, New York, p. 103 (1971).Google Scholar
- 5.Barry, B.W.:Dermatological Formulatins, Marcel Dekker, New York, p. 160 (1983).Google Scholar
- 9.Scheuplein, R.J. and Ross, L.: Effect of surfactants and solvents on the permeability,J. Soc. Cosmet. Chem. 21, 853 (1970).Google Scholar
- 13.Cooper, E.R.:Effect of Decylmethyl Sulfoxide on Skin Penetration, Mittal, K.L. and Fendler, E.J., Eds., Plenum Press, New York (1982).Google Scholar
- 23.Baglioni, P., Rivara-Minten, E., Dei, L. and Ferroni, E.: ESR study of sodium dodecyl sulfate and dodecyltrimethyl-ammonium bromide micellar solutions. Effect of ureas,J. Phys. Chem.,94, 8112 (1990).Google Scholar
- 31.Kurihara, T.: Physicochemical study of the accelerant effect of DMSO on percutaneous absorption of an antiviral drug and other chemical prototype, Ph. D. Thesis, Univ. of Michigan, Ann Arbor (1983).Google Scholar