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Transdermal Delivery of Diclofenac Using Microemulsions  

Kweon, Jang-Hoon (College of Pharmacy, Sungkyunkwan University)
Chi, Sang-Cheol (College of Pharmacy, Sungkyunkwan University)
Park, Eun-Seok (College of Pharmacy, Sungkyunkwan University)
Publication Information
Archives of Pharmacal Research / v.27, no.3, 2004 , pp. 351-356 More about this Journal
Abstract
A transdermal preparation containing diclofenac diethylammonium (DDA) was developed using an O/W microemulsion system. Of the oils tested, lauryl alcohol was chosen as the oil phase of the microemulsion, as it showed a good solubilizing capacity and excellent skin permeation rate of the drug. Pseudoternary phase diagrams were constructed to obtain the concentration range of oil, surfactant and cosurfactant for microemulsion formation, and the effect of these additives on skin permeation of DDA was evaluated with excised rat skins. The optimum formulation of the microemulsion consisted of 1.16% of DDA, 5% of lauryl alcohol, 60% of water in combination with the 34.54% of Labrasol (surfactant)/ethanol (cosurfactant) (1:2). The efficiency of formulation in the percutaneous absorption of DDA was dependent upon the contents of water and lauryl alcohol as well as Labrasol: ethanol mixing ratio. It was concluded that the percutaneous absorption of DDA from microemulsions was enhanced with increasing the lauryl alcohol and water contents, and with decreasing the Labrasol:ethanol mixing ratio in the formulation.
Keywords
Microemulsion; Diclofenac; Transdermal delivery; Topical application;
Citations & Related Records

Times Cited By Web Of Science : 28  (Related Records In Web of Science)
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1 Fevrier, F., Bobin, M. F., Lafforgue, C., and Martini, M. C., Advances in microemulsions and transepidermal penetration of tyrosine. STP Pharm. Sci., 1, 60-63 (1991)
2 Naito, S. and Tominaga, H., Percutaneous absorption of diclofenac sodium ointment. Int. J. Pharm., 24, 115-124 (1985)   DOI   ScienceOn
3 Nishihata, T., Kamada, A., Sakai, K., Takahashi, K., Matsumoto, K., Shinozaki, K., Tabata, Y., Keigami, M., Miyagi, T., and Tatsumi, N., Percutaneous absorption of diclofenac in rats and humans :aqueous gel formulation. Int. J. Pharm., 46, 1-7 (1988)   DOI   ScienceOn
4 Takahashi, K., Tamagawa, S., Katagi, T., Yoshitomi, H., Kamada, A., Rytting, J., Nishihata, T., and Mizuno, N., In vitro transport of sodium diclofenac across rat abdominal skin: Effect of selection of oleaginous component and the addition of alcohols to the vehicle. Chem. Pharm. Bull., 39, 154-158 (1991a)   DOI   PUBMED   ScienceOn
5 Touitou, E. and Fabin, B., Altered skin permation of a highly lipophilic molecule: tetrahydrocannabinol. Int. J. Pharm., 43, 17-22 (1988)   DOI   ScienceOn
6 Lasch, J., Laub, R., and Wohlarab, w., How deep do intact liposomes penetrate into human skin. J. Control. Rel., 18, 55-58 (1991)
7 Loth, H., Vehicular influence on transdermal drug penetration. Int. J. Pharm., 68, 1-10 (1991)   DOI   ScienceOn
8 Hofland, H. E. J., Bouwstra, J. A., Spies, F., Gooris, G., and Junginger, H. E., Interaction between liposomesand human skin in vitro: Poster presentation. Conference: Liposomes in DrugDelivery 21 years On, London, 12-15 (1990)
9 Iwasa, A., Irimoto, K., Kasai, S., Okuyama, H., and Nagai, T., Effect of nonionic surfactants on percutaneous absorption of diclofenac sodium. Yakuzaigaku, 51,16-21 (1991)
10 Nannipieri, E., Carelli, V., Dicolo, G., Giorgi, I., and Serafini, M. F., Vehicle influence on the permeation of highly lipophilic molecule. An in vitro technique to evaluate skin-vehicle interactions. Int. J. Cosmet. Sci., 12, 21-31 (1990)
11 Windheuser, J. J., Haslam, J. L., Caldwell, L., and Shaffer, R. D., The use of N,N-diethyl-m-toluamide to enhance dermal and transdermal delivery of drugs. J. Pharm. Sci., 71, 1211-1213 (1982)   DOI   PUBMED
12 Barry, B. W., The LPP theory of skin penetration enhancement. In Bronaugh, R. L. and Maibach, H. I. (Eds), In Vitro Percutaneous Absorption: Principles, Fundamentals, and Applications. CRS Press, Orlando, Florida, pp.165-185 (1991 )
13 Kemken, J., Ziegler, A., and Muller, B. W., Investigations into the pharmacodynamic effect of dermally administered micro-emulsions containing ${\beta}$-blockers. J. Pharm. Pharmacol., 43, 679-684 (1991)   DOI
14 Obata, Y., Takayama, K., Maitani, Y., Machida, Y., and Nagai, T., Effect of ethanol on skin permeation of nonionized and ionized diclofenac.lnt. J. Pharm., 89, 191-198 (1993)   DOI   ScienceOn
15 Takayama, K., Kikuchi, K., Obata, Y., Okabe, H., Machida, Y., and Nagai, T., Terpenes as percutaneous absorption promoters. STP Pharm. Sci., 1,.83-88(1991)
16 Knepp, V. M., Szoka, F. C., Jr and Guy, R. H., Controlled drug release from novelliposomal delivery system: II. Transdermal delivery characteristics. J. Control. Rel., 12, 25-30 (1990)   DOI   ScienceOn
17 Iwamoto, K., Kato, T., Kawahara, M., Koyama, N., Watanabe, S., Miyake, Y., and Sunamoto, J., Polysaccharide-coated oil droplets in oil-in-water emulsions as targetable carriers for lipophilic drugs. J. Pharm. Sci., 80, 219-224 (1991)   DOI   PUBMED
18 Rhee, Y.-S., Choi, J.-G., Park, E.-S., and Chi, S.-C., Transdermal delivery of ketoprofen using microemulsions. Int. J. Pharm., 228, 161-170 (2001)   DOI   PUBMED   ScienceOn
19 Takahashi, K., Tamagawa, S., Katagi, T., Yoshitomi, H., Kamada, A., Rytting, J., Nishihata, T., and Mizuno, N., In vitro percutaneous transport of sodium diclofenac and diclofenac from oleaginous vehicle. Chem. Pharm. Bull., 39, 509-511 (1991b)   DOI   PUBMED   ScienceOn
20 Obata, Y., Takayama, K., Machida, Y., and Nagai, T., Combined effect of cyclic monoterpenes and ethanol on percutaneous absorption of diclofenac sodium. Drug Design Discovery, 8, 137-144 (1991)   PUBMED
21 Menasse, R., Hodwall, R., Kractz, P. R., Pericin, J., Riester, C., Sallmann, L., Ziel, A., and Jaque, R., Scand. J. Rheumatol. Suppl., 22, 5-16 (1978)
22 Gallarate, M., Gasco,M. R. and Trotta, M., Influenceof octanoic acid on membrane permeability of timolol from solutions and from microemulsions. Acta Pharm. Technol., 34, 102-105 (1988)
23 Delgado-Charro, M. B., Iglessias-Vilas, G., Blanco-Mendez, J., Lopez-Quintela, M. A., Marty, J. P., and Guy, R. H., Delivery of hydrophilic solute through the skin from novel microemulsion systems. Eur. J. Pharm. Biopharm., 43, 37-42 (1997)   DOI   ScienceOn
24 Weiner, N. and Egbaria, K., Topical application of liposomal systems: Poster presentation. Conference: Liposomes in Drug Delivery 21 years On, London, 12-15 (1990)
25 Cappel, M. J. and Kreuter, J., Effect of nanoparticles on transdermal drug delivery. J. Microencapsul., 8, 369-374 (1991 )   DOI   PUBMED
26 Nishihata, T., Kotera, K., Nakano, Y., and Yamazaki, M., Rat percutaneous transport of diclofenac and influence of hydrogenated soya lecithin. Chem. Pharm. BUll., 35, 3801-3812 (1987)