DOI QR코드

DOI QR Code

Design of Transdermal Delivery System Using New Film-Forming Agents

신규 필름형성제를 이용한 경피흡수제제의 설계

  • 최양규 (태평양기술연구원 의약건강연구소) ;
  • 김영소 (태평양기술연구원 의약건강연구소) ;
  • 김정주 (태평양기술연구원 의약건강연구소) ;
  • 심영철 (태평양기술연구원 의약건강연구소)
  • Published : 2003.09.20

Abstract

In order to develop a film-forming transdermal drug delivery system, polyurethane (PU) based on poly(ethylene glycol) and poly(tetramethylene oxide) was synthesized and characterized. The synthesized PU was blended with Gantrez ES 225 (GT) to improve the adhesion property of film-forming agent to the skin. When film-forming gel formulation containing 3% ketoprofen (KP) was applied, transparent thin film was obtained within 5 minutes and adhered to the skin for 8 hours. In vitro percutaneous absortion studies were performed to determine the rate of ketoprofen absorption through guinea pig skin. A prominent effect of limonene on the skin permeability of ketoprofen was observed among the various skin permeation enhancers investigated. Considering mechanica properties of film and skin permeability of ketoprofen, 2% of limonene was optimal content in the film forming transdermal formulation.

Keywords

References

  1. A.F. Kydonieus, Fundamental of transdermal drug delivery : In Transdermal delivery of drugs, Vol. I, A.F. Kydonieus and B. Berner (Ed.), CRS Press, Florida, U.S.A., pp.3-28 (1987)
  2. R.H. Guy, Current status and future prospects of transdermal drug delivery, Pharm. Res., 13, 1765-1769 (1996) https://doi.org/10.1023/A:1016060403438
  3. T.K. Ghosh and W.R. Pfister, Transdermal and topical delivery systems : An overview and future trends : In Transdermal and topical drug delivery system, T.K Ghosh, W.R. Pfister and S.I. Yum (Ed.), Interpharm Press, Buffalo Grove, U.S.A., pp. 1-32 (1997)
  4. Y.W. Chien, Advances in transdermal systemic medication: In Trandermal controlled systemic medication, Y.W Chien (Ed.), Marcel Dekker, New York, U.S.A., pp. 1-21 (1987)
  5. Y. Yamaguchi, T. Usami, H. Natsume, T. Aoyagi, Y. Nagase, K. Sugibayashi and Y. Morimoto, Evaluation of skin permeability of drugs by newly prepared polymer membranes, Chem. Pharm, Bull., 45, 537-541 (1997) https://doi.org/10.1248/cpb.45.537
  6. S. Magdassi and E. Tuoitou, Cosmeceutics and delivery system : In Novel cosmetic delivery systems, S. Magdassi and E. Tuoitou (Ed.), Marcel Dekker, New York, U.S.A., pp. 1-7 (1999)
  7. S. Venkatrama, R. Gele, Skin adhesive and skin adhesion 1. Transdermal drug delivery systems, Biomaterials, 19, 1119-1136 (1998) https://doi.org/10.1016/S0142-9612(98)00020-9
  8. P.R. Rao and P.V. Diwan, Formulation and in vitro evaluation of polymeric films of diltiazem hydrochloride and indomethacin for transdermal administration, Drug Dev. Ind. Pharm., 24(4), 327-336 (1998) https://doi.org/10.3109/03639049809085627
  9. lD. Dell, Film-forming composition containing an antimicrobial agent and methods, US patent 4,542,012
  10. S.Y. Lin, C.J. Lee and Y.Y Lin, The effect of plasticizers on compatibility, mechanical properties, and adhesion strength of drug-free Eudragit E films, Pharm. Res., 8, 1137-1143 (1991) https://doi.org/10.1023/A:1015850301214
  11. S.Y. Lin, C.J. Lee and Y.Y Lin, Drug-polymer interaction affecting the mechanical properties, adhesion strength and release kinetics of piroxicam-loaded Eudragit E film plasticized with different plasticizers, J. Controlled Release, 33, 375-381 (1995) https://doi.org/10.1016/0168-3659(94)00109-8
  12. E.Y. Hosny, S.S. Abdel Hady and E.M. Niazy, Effect of film composition and various penetration enhancers concentrations on Prazosin release from acrylic polymeric film, Pharm. Acta. Helv., 72, 247-245 (1998) https://doi.org/10.1016/S0031-6865(97)00024-1
  13. J.C. Sciarra and S.P. Patel, In vitro release of therapeutically active ingredients from polymer matrixes, J. Pharm. Sci., 65, 1519-1522 (1976) https://doi.org/10.1002/jps.2600651025
  14. R.K. Chang, C.H. Hsiao and J.R. Robinson, A review of aqueous coating techniques and preliminary data on release from a theophylline product., Pharm. Technol., 11, 56-68 (1987)
  15. L.C. Li and N.T. Vu, An in vitro evaluation of silicon elastomer latex for topical drug delivery, J. Pharm. Pharmacol., 47, 447-452 (1995) https://doi.org/10.1111/j.2042-7158.1995.tb05827.x
  16. Brochure of Gantrez ES Monester Resins (ISP Technologies, Inc.): Tests conducted by Industrial Biology Research and Testing Laboratories, Inc. according to procedures described in the regulations for the Federal Hazardous Substances Act
  17. Y.J. Li, T. Yokawa, K.H. Matthews, T.M. Chen, Y.F. Wang, M. Kodama and T. Nakaya, Synthesis and blood compatibility evaluation of segmented polyurethanes based on cholesterol and phosphatidylcholine analogous moieties, Biomaterials, 17, 2179-2189 (1996) https://doi.org/10.1016/0142-9612(96)00048-8
  18. P.N. Lan, S. Corneille, E. Schacht, M. Davies and A. Shard, Synthesis and characterization of segmented polyurethanes based on amphiphilic polyether diols, Biomaterials, 17, 2273-2280 (1996) https://doi.org/10.1016/0142-9612(96)00056-7
  19. Test Methods for pressure sensitive adhesive tapes (10th edition), Pressure Sensitive adhesive Tape Council, Chicago, U.S.A., pp.23-24 (1992)
  20. S.I. Yum, E. Lim, L.Taskovich and F. Theeuwes, Permeation enhancement with ethanol : Mechanism of action through skin: In Durg permeation enhancement theory and application, D.S. Hsieh (Ed.), Marcel Dekker, New York, U.S.A., pp. 143-170 (1994)
  21. N. Buyuktimkin, S. Buyuktimkin and J. H. Rytting, Chemical means of transdermal drug permeation enhancement : In Transdermal and topical drug delivery system, T.K. Ghosh, W.R. Pfister and S.I. Yum (Ed.), Interpharm Press, Buffalo Grove, U.S.A., pp. 357-475 (1997)
  22. Y. Nakamura, K. Takayama, K. Higashiyama, T. Suzuki and T. Nagai, Promoting effect of O-ethylmenthol on the percutaneous absorption of ketoprofen, Int. J. Pharm., 145,29-36 (1996) https://doi.org/10.1016/S0378-5173(96)04749-7
  23. H.O. Ho, L.C. Chen, H.M. Lin and M.T. Sheu, Penetration enhancement by menthol combined with a solubilization effect in a mixed solvent system, J.Controlled Release, 51, 301-311 (1998) https://doi.org/10.1016/S0168-3659(97)00184-3
  24. O. Shirakura, A. Ohshima, S. Tsunemi, S. Ishimaru, T. Sakaguchi and K. Takayama, Synergistic effect of d-limonene and ethanol on the transdermal permeation of NB-818, Drug Dev. Ind. Pharm., 21, 411-25 (1995) https://doi.org/10.3109/03639049509026632
  25. K. Takayama and T. Nagai, Limonene and related compounds as potential skin penetration promoters, Drug Dev. Ind. Pharm., 20, 677-684 (1994) https://doi.org/10.3109/03639049409038325