Transdermal delivery of Risedronate using the pressure sensitive adhesive patch with various permeation enhancers

Authors

Abstract

Risedronate monosodium (RIS) is widely used for treating bone disorders. Although RIS is commonly available in the oral drug market, it has side effects such as gastrointestinal troubles, abdominal pain, and severe esophageal irritation. To address these issues associated with oral administration, a pressure-sensitive adhesive patch of RIS was developed for the transdermal delivery, and its penetration rate was evaluated using hairless mouse skin. To increase the permeation of RIS, diethylenetriamine (DETA) was used as a solubilizer and fatty acids were used as enhancers. The cumulative amount of RIS penetrating through the mouse skin using various fatty acids, such as lauric acid (LA), capric acid (C10), caprylic acid (C8), linoleic acid (LiA), and oleic acid (OA) in the patches, were 68.21 ± 17.71 μg, 2.25 ± 2.11 μg, 2.79 ± 0.79 μg, 38.86 ± 3.14 μg, and 41.76 ± 2.17 μg, respectively, compared to 3.38 ± 1.34 μg in the case of the RIS patch without an enhancer. The patch formulation with a weight ratio of 6:1:1 (pressure-sensitive adhesive Duro-Tak® 87-202A, 10% (w/w) RIS, and LA) showed the highest permeation efficiency, demonstrating the effectiveness of enhancers for the transdermal drug delivery patch of RIS

Keywords: Risedronate, Transdermal delivery, pressure adhesive patch, enhancers, fatty acids.

Keywords:

Risedronate, Transdermal delivery, pressure adhesive patch, enhancers, fatty acids

DOI

https://doi.org/10.22270/jddt.v15i6.7195

Author Biography

So Hee Nam , Associate Professor, College of Pharmacy, Dongduk Women’s University, Hwarang-ro 13, Seongbuk-gu, Seoul 02748, Republic of Korea

Associate Professor, College of Pharmacy, Dongduk Women’s University, Hwarang-ro 13, Seongbuk-gu, Seoul 02748, Republic of Korea

References

1. Russell RGG, Xia Z, Dunford JE, Oppermann U, Kwaasi A, Hulley PA, et al. An update on mechanisms of action and how these relate to clinical efficacy. Ann NY Acad Sci. 2007;1117:209-57. https://doi.org/10.1196/annals.1402.089 PMid:18056045

2. McClung M, Geusens P. Review of risedronate in the treatment of osteoporosis. Expert Opinion on pharmacotherapy. 2001;2(12):2011-25. https://doi.org/10.1517/14656566.2.12.2011

PMid:11825332

3. Sakuma S, Tanno FK, Masaoka Y, Kataoka M, Kozaki T, Kamaguchi R, et al. Effect of administration site in the gastrointestinal tract on bioavailability of poorly absorbed drugs taken after a meal. Journal of Controlled Release. 2007;118(1):59-64. https://doi.org/10.1016/j.jconrel.2006.12.016 PMid:17250919

4. Lin J. Bisphosphonates: a review of their pharmacokinetic properties. Bone. 1996;18(2):75-85. https://doi.org/10.1016/8756-3282(95)00445-9 PMid:8833200

5. Abrahamsen B. Adverse Effects of Bisphosphonates. Calcified Tissue International. 2010;86(6):421-35. https://doi.org/10.1007/s00223-010-9364-1 PMid:20407762

6. Abrahamsen B. Adverse effects of bisphosphonates. Calcified tissue international. 2010;86:421-35. https://doi.org/10.1007/s00223-010-9364-1 PMid:20407762

7. Guy R. Transdermal Drug Delivery. In: Schäfer-Korting M, editor. Drug Delivery. Handbook of Experimental Pharmacology. 197: Springer Berlin Heidelberg; 2010. p. 399-410. https://doi.org/10.1007/978-3-642-00477-3_13 PMid:20217537

8. Jeong WY, Kwon M, Choi HE, Kim KS. Recent advances in transdermal drug delivery systems: A review. Biomaterials research. 2021;25(1):24. https://doi.org/10.1186/s40824-021-00226-6 PMid:34321111 PMCid:PMC8317283

9. Czech Z, Kurzawa R. Acrylic pressure-sensitive adhesive for transdermal drug delivery systems. Journal of Applied Polymer Science. 2007;106(4):2398-404. https://doi.org/10.1002/app.26751

10. Tsuji K, Mitsutake S, Ishikawa J, Takagi Y, Akiyama M, Shimizu H, et al. Dietary glucosylceramide improves skin barrier function in hairless mice. Journal of Dermatological Science. 2006;44(2):101-7. https://doi.org/10.1016/j.jdermsci.2006.08.005 PMid:17000082

11. Goldstein AM, Abramovits W. Ceramides and the stratum corneum: structure, function, and new methods to promote repair. International Journal of Dermatology. 2003;42(4):256-9. https://doi.org/10.1046/j.1365-4362.2003.01507.x PMid:12694488

12. Prausnitz MR, Elias PM, Franz TJ, Schmuth M, Tsai J-C, Menon GK, et al. Skin barrier and transdermal drug delivery. Dermatology. 2012;3(18):2065-73.

13. Nam SH, Xu YJ, Nam H, Jin G-w, Jeong Y, An S, et al. Ion pairs of risedronate for transdermal delivery and enhanced permeation rate on hairless mouse skin. International journal of pharmaceutics. 2011;419(1-2):114-20. https://doi.org/10.1016/j.ijpharm.2011.07.027 PMid:21807082

14. Schultz C. Prodrugs of biologically active phosphate esters. Bioorganic & medicinal chemistry. 2003;11(6):885-98. https://doi.org/10.1016/S0968-0896(02)00552-7 PMid:12614874

15. Marcus Y, Hefter G. Ion pairing. Chemical reviews. 2006;106(11):4585-621. https://doi.org/10.1021/cr040087x PMid:17091929

16. Cristofoli M, Kung C-P, Hadgraft J, Lane ME, Sil BC. Ion pairs for transdermal and dermal drug delivery: a review. Pharmaceutics. 2021;13(6):909. https://doi.org/10.3390/pharmaceutics13060909 PMid:34202939 PMCid:PMC8234378

17. Wang M, Fang L, Ren C, Li T. Effect of ion-pairing and enhancers on scutellarin skin permeability. Journal of Pharmacy and Pharmacology. 2008;60(4):429-35. https://doi.org/10.1211/jpp.60.4.0004 PMid:18380914

18. Barry BW. Mode of action of penetration enhancers in human skin. Journal of Controlled Release. 1987;6(1):85-97. https://doi.org/10.1016/0168-3659(87)90066-6

19. Lane ME. Skin penetration enhancers. International journal of pharmaceutics. 2013;447(1-2):12-21. https://doi.org/10.1016/j.ijpharm.2013.02.040 PMid:23462366

20. Lopes LB, J Garcia MT, LB Bentley MV. Chemical penetration enhancers. Therapeutic delivery. 2015;6(9):1053-61. https://doi.org/10.4155/tde.15.61 PMid:26458111

21. Golden GM, McKie JE, Potts RO. Role of stratum corneum lipid fluidity in transdermal drug flux. Journal of Pharmaceutical Sciences. 1987;76(1):25-8. https://doi.org/10.1002/jps.2600760108 PMid:3585718

22. Ibrahim SA, Li SK. Efficiency of fatty acids as chemical penetration enhancers: mechanisms and structure enhancement relationship. Pharmaceutical research. 2010;27:115-25. https://doi.org/10.1007/s11095-009-9985-0 PMid:19911256 PMCid:PMC2898574

23. Tan HS, Pfister WR. Pressure-sensitive adhesives for transdermal drug delivery systems. Pharmaceutical Science & Technology Today. 1999;2(2):60-9. https://doi.org/10.1016/S1461-5347(99)00119-4 PMid:10234208

24. Walters KA, Lane ME. Dermal and Transdermal Drug Delivery Systems: An Overview and Recent Advancements. Dermal Drug Delivery. 2020:1-60. https://doi.org/10.1201/9781315374215-1

25. Sinha VR, Kaur MP. Permeation Enhancers for Transdermal Drug Delivery. Drug Development and Industrial Pharmacy. 2000;26(11):1131-40. https://doi.org/10.1081/DDC-100100984 PMid:11068686

26. Nam SH, Xu YJ, Nam H, Jin G-w, Jeong Y, An S, et al. Ion pairs of risedronate for transdermal delivery and enhanced permeation rate on hairless mouse skin. International Journal of Pharmaceutics. 2011;419(1-2):114-20. https://doi.org/10.1016/j.ijpharm.2011.07.027 PMid:21807082

27. Whang J, Gwak H. Effects of amines on percutaneous absorption of alendronate. Drug Development and Industrial Pharmacy. 2011;37(5):491-7. https://doi.org/10.3109/03639045.2010.525237 PMid:21126206

28. Williams AC, Barry BW. Penetration enhancers. Advanced Drug Delivery Reviews. 2012;64, Supplement(0):128-37. https://doi.org/10.1016/j.addr.2012.09.032

29. Walker RB, Smith EW. The role of percutaneous penetration enhancers. Advanced Drug Delivery Reviews. 1996;18(3):295-301. https://doi.org/10.1016/0169-409X(95)00078-L

30. Aungst B, Blake J, Hussain M. Contributions of Drug Solubilization, Partitioning, Barrier Disruption, and Solvent Permeation to the Enhancement of Skin Permeation of Various Compounds with Fatty Acids and Amines. Pharmaceutical Research. 1990;7(7):712-8. https://doi.org/10.1023/A:1015859320604 PMid:2395798

Published

2025-06-15
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How to Cite

1.
NAM SH. Transdermal delivery of Risedronate using the pressure sensitive adhesive patch with various permeation enhancers. J. Drug Delivery Ther. [Internet]. 2025 Jun. 15 [cited 2026 Jan. 23];15(6):90-5. Available from: https://jddtonline.info/index.php/jddt/article/view/7195

How to Cite

1.
NAM SH. Transdermal delivery of Risedronate using the pressure sensitive adhesive patch with various permeation enhancers. J. Drug Delivery Ther. [Internet]. 2025 Jun. 15 [cited 2026 Jan. 23];15(6):90-5. Available from: https://jddtonline.info/index.php/jddt/article/view/7195