Browse > Article

Formulation of Microemulsion Systems for Transdermal Delivery of Aceclofenac  

Lee, Jae-Hwi (Division of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University)
Lee, Yoon-Jin (Division of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University)
Kim, Jong-Seok (Division of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University)
Yoon, Mi-Kyeong (Division of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University)
Choi, Young-Wook (Division of Pharmaceutical Sciences, College of Pharmacy, Chung-Ang University)
Publication Information
Archives of Pharmacal Research / v.28, no.9, 2005 , pp. 1097-1102 More about this Journal
Abstract
An O/W microemulsion system was developed to enhance the skin permeability of ace-clofenac. Of the oils studied, Labrafil? M 1944 CS was chosen as the oil phase: of the microemulson, as it showed a good solubilizing capacity. Pseudo-ternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, Cremophor ELP, and co-surfactant, ethanol, for micoemulsion formation. Eight different formulations with various values of oil of $6-30\%$, water of $0-80\%$, and the mixture of surfactant and co-surfactant (at the ratio of 2) of $14-70\%$. The in vitro transdermal permeability of aceclofenac from the microemulsions was evaluated using Franz diffusion cells mounted with rat skin. The level of aceclofenac permeated was analyzed by HPLC and the droplet size' of the microemulsions was characterized using a Zetasizer Nano-ZS. Terpenes were added to the microemulsions at a level of $5\%$, and their effects on the skin permeation of aceclofenac were investigated. The mean diameters of the microemulsions ranged between approximately $10\~100nm$, and the skin permeability of the aceclofenac incorporated into the microemulsion systems was 5-fold higher than that of the ethanol vehicle. Of the various terpenes added, limonene had the best enhancing ability. These results indicate that the microemulsion pystem studied is a promising tool for the percutaneous delivery of aceclofenac.
Keywords
Aceclofenac; Microemulsions; Permeation enhancer; Transdermal delivery; Terpenes;
Citations & Related Records

Times Cited By Web Of Science : 28  (Related Records In Web of Science)
Times Cited By SCOPUS : 27
연도 인용수 순위
1 Cornwell, P. A. and Barry, B. W., Sesquiterpene components of volatile oils as skin penetration enhancers for the hydrophilic permeant 5-fluorouracil. J. Pharm. Pharmacol., 46, 261-269 (1994)   DOI   ScienceOn
2 Gasco, M. R., In: Microemulsions in the Pharmaceutical Field: Persperctives and Applications, Industrial Applications of Microemulsions, Marcel Dekker Inc, New York. 97-122 (1997)
3 Kobayashi, D., Matsuzawa, T., Sugibayashi, K., Morimoto, Y., Kobayashi, M., and Kimura, M., Feasibility of use of several cardiovascular agents in transdermal therapeutic systems with -menthol-ethanol system on hairless rat and human skin. Biol. Pharm. Bull., 16, 254-258 (1993)   DOI   ScienceOn
4 Lawrence, M. J. and Rees, G. D., Microemulsion-based media as novel drug delivery systems. Adv. Drug Deliv. Rev., 45, 89-121 (2000)   DOI   ScienceOn
5 Williams, A. C. and Barry, B. W., Skin absorption enhancers. Crit. Rev. Ther. Drug Carrier Syst., 9, 305-353 (1992)
6 Arellano, S., Santoyo, S., Martin, C., and Ygartua, P., Enhancing effect of terpenes on the in vitro percutaneous absorption of diclofenac sodium. Int. J. Pharm., 130, 141-145 (1996)   DOI   ScienceOn
7 Moghimi, H. R., Williams, A. C., and Barry, B. W., A lamellar matrix model for stratum corneum intercellular lipids. V. Effects of terpene penetration enhancers on the structure and thermal behaviour of the matrix. Int. J. Pharm., 146, 41–54 (1997)   DOI   ScienceOn
8 Yamazaki, R., Kawai, S., Matsuzaki, T., Kaneda, N., Hashimoto, S., Yokokura, T., Okamoto, R., Koshino, T., and Mizushima, Y., Aceclofenac blocks prostaglandin $E_{2}$ production following its intracellular conversion into cyclooxygenase inhibitors. Eur. J. Pharmacol., 329, 181-187 (1997)   DOI
9 Buyuktimkin, N., Buyuktimkin, S., and Rytting, J. H., Chemical means of transdermal drug permeation enhancement. In: Ghosh, T. K., Pfister, W. R, Yum, S. I. (Eds.), Transdermal and Topical Drug Delivery Systems, Interpharm Press, IL pp. 357-475 (1997)
10 Gonzalez, E., Cruz, C., Nicolas, R., Egido, J., and Herrero-Beaumont, G., Long-term effect of nonsteroidal antiinflammatory drugs on the production of cytokines and other inflammatory mediators by blood cells of patients with osteoarthritis. Agents Actions, 41, 171-178 (1994)   DOI   ScienceOn
11 Bennett, K. E., Hatfield, J. C., Davis, H. T., Macosko, C. W., and Scriven, L. E., Viscosity and conductivity of microemulsions. In: Robb, I. D. (Ed.), Microemulsions. Plenum Press, New York, pp. 65-84. (1982)
12 Williams, A. C. and Barry, B. W., Terpenes and the lipid–proteinpartitioning theory of skin penetration enhancement. Pharm. Res., 8, 17-24 (1991a)   DOI   ScienceOn
13 Cornwell, P. A., Barry, B. W., Bouwstra, J. A., and Gooris, G. S., Modes of action of terpene penetration enhancers in human skin; differential scanning calorimetry, small-angle X-ray diffraction and enhancer uptake studies. Int. J. Pharm., 127, 9-26 (1996)   DOI   ScienceOn
14 Williams, A. C. and Barry, B. W., The enhancement index concept applied to terpene penetration enhancers for human skin and model lipophilic (oestradiol) and hydrophilic (5-fluorouracil) drugs. Int. J. Pharm., 74, 157-168 (1991b)   DOI   ScienceOn
15 Tenjarla, S., Microemulsions: an overview and pharmaceutical applications. Crit. Rev. Ther. Drug Carrier Syst., 16, 461-521 (1999)