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Transdermal Delivery of Estradiol and Norethindrone Acetate: Effect of Vehicles and Pressure Sensitive Adhesive Matrix

  • Published : 2005.06.20

Abstract

Addition of 30% propylene glycol was required to maintain sink condition in the evaluation of percutaneous absorption of estradiol and norethindrone acetate. The permeability of estradiol was higher in silicone and SIS adhesives. However, estradiol was crystallized in silicone, SIS, and SBS adhesive matrix. The permeability ratio of estradiol or norethindrone acetate from acrylic pressure sensitive adhesives varied widely depending on the functional group of the acrylic adhesives. PEO grafting to acrylic adhesive seemed to change physicochemical property of acrylic adhesive and increased the permeability of estradiol and norethindrone acetate significantly. On the contrary, highly cross-linked enhancer compatible acrylic adhesive decreased the permeability of both estradiol and norethindrone acetate. $Span^{\circledR}$ 20 provided the highest enhancing effect on the permeability of both estradiol and norethindrone acetate followed by oleic acid and $Crovol^{\circledR}$ EP40. The permeability of the drugs from the developed system was comparable to that from commercial $Combitran^{\circledR}$, although significantly lower amount of estradiol and norethindrone acetate were loaded in the developed system.

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References

  1. C. Grant, A. Gray, R. Paoletti, et al., Hormone replacement therapy, The Lancet, 354, 152-155 (1999) https://doi.org/10.1016/S0140-6736(99)06570-8
  2. E. Grodstein, M.J. Stampfer, J.E. Manson, G.A. Colditz, W.C. Willett, B. Rosner, EE. Speizer and C.H. Hennekens, Postmenopausal estrogen and progestin use and the risk of cardiovascular disease, N. Engl. J. Med. 335, 453-461 (1996) https://doi.org/10.1056/NEJM199608153350701
  3. C. Castelo-Branco, M.J. Martinez de Osaba, F. Pons and J. Gonzalez-Merlo, The effect of hormone replacement therapy on postmenopausal bone loss, Eur. J. Obstetr. Gynecol. Reprod. Biol. 44, 131-136 (1992) https://doi.org/10.1016/0028-2243(92)90058-7
  4. E. Barrett-Connor and D. Gray, Hormone replacement therapy, heart disease, and other considerations, Annu. Rev. Public health, 19, 55-72 (1998) https://doi.org/10.1146/annurev.publhealth.19.1.55
  5. M.J. Stampfer, G.A. Colditz, W.C. Willett, J.E. Manson, B. Rosner, E.E. Speizer and C.H. Hennekens, Postmenopausal estrogen therapy and cardiovascular disease. Ten-year follow-up from the nurses' health study, N Engl. J. Med. 325, 756-762 (1991) https://doi.org/10.1056/NEJM199109123251102
  6. H.K. Genant, J. Lucas, S. Weiss, M. Akin, R. Enkey, H. Mcnaney-Flint, R. Downs, J. Mortola, N. Watts, H.M. Yang, N. Banar, J.J. Brennan and J.C. Nolan, Low-dose esterified estrogen therapy: effects on bone, plasma estradiol concentrations, endometrium, and lipid levels. Estratab/Osteoporosis Study, Arch. Intern. Med. 157, 2609-2615 (1997) https://doi.org/10.1001/archinte.157.22.2609
  7. T. Holst and B. Salbach, Efficacy of a new 7 -day transdermal sequential estradiol/levonorgestrel patch in women, Maturitas, 41, 231-242 (2002) https://doi.org/10.1016/S0378-5122(01)00297-3
  8. R. Rossi, G. Origliani and M.G Modena, Transdermal 17-betaestradiol and risk of developing type 2 diabetes in a population of healthy, nonobese postmenopausal women, Diabetes Care. 27, 645-649 (2004) https://doi.org/10.2337/diacare.27.3.645
  9. M.S. Post, M.J. van der Moorenvan, W.M. Baal, M.A. Blankenstein, H.M. Merkus, M.Y. Kroeks, H.R. Franke, P. Kenemans and CD. Stehouwer, Effects of low-dose oral and transdermal estrogen replacement therapy on hemostatic factors in healthy postmenopausal women: A randomized placebo-controlled study, Am. J. Obstet. Gynecoz. 189, 1221-1227 (2003) https://doi.org/10.1067/S0002-9378(03)00599-4
  10. E. Weiderpass, H.O. Adami, J.A. Baron, C. Magnusson, R. Bergstrom, A. Lindgren, N. Correia and J. Persson, Risk of endometrial cancer following estrogen replacement with and without progestins, J. Natl. Cancer Inst. 91, 1131-1137 (1999) https://doi.org/10.1093/jnci/91.13.1131
  11. M. Hori, et al., Classification of percutaneous penetration enhancers. In: R.L. Bronaugh, H.I. Maibach Editors, Percutaneous Absorption: Mechanisms, Methodology, Drug Delivery, Marcel Dekker, New York, USA, pp. 197-211 (1989)
  12. J.-H. Kim, C.H. Lee and H.-K. Choi, Transdennal delivery of physostigmine: Effects of enhancers and pressure sensitive adhesives, Drug Dev. Ind. Pharm., 28, 833-839 (2002) https://doi.org/10.1081/DDC-120005629
  13. T. Kokubo, K. Sugibayashi and Y. Morimoto, Interaction between drugs and pressure-sensitive adhesive in transdermal therapeutic systems, Pharm. Res. 11, 104-107 (1994) https://doi.org/10.1023/A:1018906013527
  14. J.-H. Kim, Y.-J. Cho and H.-K. Choi, Effect of vehicles and pressure sensitive adhesives in the permeation for tacrine across hairless mouse skin, Int. J. Pharm. 196, 105-113 (2000) https://doi.org/10.1016/S0378-5173(99)00449-4
  15. H.-K. Choi and J.T. Angello, Mathematical analysis and optimization of flow-through diffusion cell system. Pharm. Res. 11, 595-599 (1994) https://doi.org/10.1023/A:1018991221647
  16. X. Ma, J. Taw and C.M. Chiang, Control of drug crystallization in transdermal matrix system, Int. J. Pharm. 142, 115-119 (1996) https://doi.org/10.1016/0378-5173(96)04647-9
  17. D.R. Friend and P. Catz, Effect of cosolvents on ethyl acetate enhanced percutaneous absorption of levonorgestrel, J. Control. Release, 12, 171-180 (1990) https://doi.org/10.1016/0168-3659(90)90093-9
  18. G.S. Chen, D.O. Kim and Y.W. Chien, Dual-controlled transdermal delivery of levonorgestrel and estradiol: enhanced permeation and modulated delivery, J. Control. Release, 34, 129-143 (1995) https://doi.org/10.1016/0168-3659(95)00005-S
  19. L.K. Pershing, G.E. Parry and L.D. Lambert, Disparity of in vitro and in vivo oleic acid-enhanced ${\beta}$-estradiol percutaneous absorption across human skin, Pharm. Res. 10, 1745-1750 (1993) https://doi.org/10.1023/A:1018974131236