Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Effect of Enhancers and Pressure Sensitive Adhesives on the Transdermal Delivery of Fentanyl

  • Lee, Ji-Young (BK21 Project Team, College of Pharmacy, Chosun University) ;
  • Jang, Joon-Ho (BK21 Project Team, College of Pharmacy, Chosun University) ;
  • Choi, Hoo-Kyun (BK21 Project Team, College of Pharmacy, Chosun University)
  • Published : 2008.08.20
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Abstract

The purpose of this study was to investigate the feasibility of developing transdermal drug delivery system (TDDS) for fentanyl used for the management of chronic cancer pain. The effect of type of pressure sensitive adhesive on the permeation of fentanyl from polyisobutylene (PIB), silicone and acrylic adhesive was evaluated. Due to the good adhesive force and relatively steady flux for 3 days, both acrylic and PIB adhesives were chosen for further study. The permeation rate of fentanyl was the highest from acrylic adhesive with hydroxyl functional group. Permeation rate increased linearly as the concentration of fentanyl in acrylic adhesive was increased from 2.5% to 10%. In case of PIB adhesive, crystals of fentanyl were developed above 5% drug load. $Crovol^{(R)}$ A40, $Crovol^{(R)}$ PK40 and Plurol $oleique^{(R)}$ provided higher flux of fentanyl.

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References

  1. M.E. Mouedden and T.F. Meert, The impact of the opioids fentanyl and morphine on nociception and bone destruction in a murine model of bone cancer pain, Pharmacol. Biochem. Behav., 87, 30-40 (2007) https://doi.org/10.1016/j.pbb.2007.03.017
  2. B. Ebert, C. Thorkildsen, S. Andersen, L. Christrup, L. and Hfeds, H., Opioid analgesics as noncompetitive N-methyl-daspartate (NMDA) antagonists-Synthesis and identification of a major metabolite, Biochem. Pharmacol., 56, 553-559 (1998) https://doi.org/10.1016/S0006-2952(98)00088-4
  3. T.H. Stanley, Fentanyl, J. Pain Symptom. Manage., 29, S67-S71 (2005) https://doi.org/10.1016/j.jpainsymman.2005.01.009
  4. S.D. Roy, M. Gutierrez, G.L. Flynn and G.W. Clear, Controlled transdermal delivery of fentanyl: Characterizations of pressure- sensitive adhesives for matrix patch design, J. Pharm. Sci., 85, 491-495 (1996) https://doi.org/10.1021/js950415w
  5. R. Freynhagen, P. Busche, R. Sabatowski, C. Konrad and S. Grond, Switching from reservoir to matrix systems for the transdermal delivery of fentanyl: A prospective, multicenter pilot study in outpatients with chronic pain, J. Pain Symptom. Manage., 30, 289-297 (2005) https://doi.org/10.1016/j.jpainsymman.2005.03.015
  6. T. Kotyla, F. Kuo, V. Moolchandani, T. Wilson and R. Nicolosi, Increased bioavailability of a transdermal application of a nano-sized emulsion preparation Int. J. Pharm., 347, 144-148 (2008) https://doi.org/10.1016/j.ijpharm.2007.06.045
  7. M.H. Qvist, U. Hoeck, B. Kreilgaard, F. Madsen and S. Frokjaer, Release of chemical permeation enhancers from drug-in-adhesive transdermal patches, Int. J. Pharm., 231, 253-263 (2002) https://doi.org/10.1016/S0378-5173(01)00893-6
  8. I. Alberti, Y.N. Kalia, A. Naik, J.D. Bonny and R.H. Guy, In vivo assessment of enhanced topical delivery of terbinafine to human stratum corneum J. Control. Release, 71, 319-327 (2001) https://doi.org/10.1016/S0168-3659(01)00244-9
  9. M. Guyot and F. Fawaz, Design and in vitro evaluation of adhesive matrix for transdermal delivery of propranolol, Int. J. Pharm., 204, 171-182 (2000) https://doi.org/10.1016/S0378-5173(00)00494-4
  10. Y.J. Cho and H.K. Choi, Enhancement of percutaneous absorption of ketoprofen: effect of vehicles and adhesive matrix, Int. J. Pharm., 169, 95-104 (1998) https://doi.org/10.1016/S0378-5173(98)00115-X
  11. H.S. Tan and W.R. Pfister, Pressure-sensitive adhesives for transdermal drug delivery systems, Pharm. Sci. Technol. Today, 2, 60-69 (1999) https://doi.org/10.1016/S1461-5347(99)00119-4
  12. M. Bach and B.C. Lippold, Percutaneous penetration enhancement and its qualification, Eur. J. Pharm. Biopharm., 46, 1-13 (1998) https://doi.org/10.1016/S0939-6411(97)00149-5
  13. J.-H. Kim, Y.-J. Cho and H.-K. Choi, Effect of vehicles and pressure sensitive adhesives on the permeation of tacrine across hairless mouse skin. Int. J. Pharm., 196, 105-113 (2000) https://doi.org/10.1016/S0378-5173(99)00449-4
  14. T.M. Suhonen, J.A. Bouwstra and A. Urtti, Chemical enhancement of percutaneous absorption in relation to stratum corneum structural alterations, J. Control. Release, 59, 149-161 (1999) https://doi.org/10.1016/S0168-3659(98)00187-4
  15. A.C. Williams and B.W. Barry, Penetration enhancers, Adv. Drug Delivery., 56, 603-618 (2004) https://doi.org/10.1016/j.addr.2003.10.025
  16. P. Minghetti, A. Casiraghi, F. Cilurzo and L. Montanari, Development of local patches containing melilot extract and ex vivoin vivo evaluation of skin permeation, Eur. J. Pharm. Biopharm., 10, 111-117 (2000)