Mekanisme Kerja Peningkat Penetrasi Golongan Asam Lemak Pada Sediaan Transdermal: Review.

Vini Almira, Sabrina Dahlizar, Supandi Supandi

Abstract


Sediaan transdermal merupakan sediaan yang diaplikasikan pada permukaan kulit dan dirancang untuk dapat mengantarkan obat melalui kulit ke sirkulasi sistemik. Untuk dapat memberikan efek terapeutik, suatu sediaan transdermal harus mampu menembus lapisan kulit. Penetrasi obat sediaan transdermal ke dalam kulit dapat ditingkatkan dengan menambahkan peningkat penetrasi. Asam lemak merupakan peningkat penetrasi kimia yang dapat meningkatkan permeasi obat hidrofilik dan lipofilik. Penelitian ini menggunakan metode systematic literature review (SLR) dan membahas artikel penelitian selama 15 tahun terakhir yang membahas tentang penggunaan peningkat penetrasi golongan asam lemak dalam sediaan transdermal. Diperoleh hasil sebanyak 30 artikel yang memenuhi kriteria. Hasil penelitian ini membuktikan bahwa asam lemak terbukti dapat meningkatkan permeasi obat hidrofilik maupun lipofil pada sediaan transdermal. Faktor yang mempengaruhi kemampuan peningkatan penetrasi asam lemak diantaranya variasi asam lemak, konsentrasi asam lemak yang digunakan dan kombinasi asam lemak dengan peningkat penetrasi lain. Asam lemak tak jenuh lebih efektif meningkatkan permeasi dibandingkan dengan asam lemak jenuh dan asam lemak yang paling banyak digunakan untuk meningkatkan permeasi adalah asam oleat.


References


Ahad, A. et al. (2009) “Chemical penetration enhancers: A patent review,” Expert Opinion on Therapeutic Patents, 19(7), hal. 969–988. doi: 10.1517/13543770902989983.

Alkilani, A. Z., McCrudden, M. T. C. dan Donnelly, R. F. (2015) “Transdermal drug delivery: Innovative pharmaceutical developments based on disruption of the barrier properties of the stratum corneum,” Pharmaceutics, 7(4), hal. 438–470. doi: 10.3390/pharmaceutics7040438.

Ammar, H. et al. (2006) “A Transdermal Delivery System for Glipizide,” Current Drug Delivery, 3(3), hal. 333–341. doi: 10.2174/156720106777731037.

Bolzinger, M. et al. (2012) “Penetration of drugs through skin, a complex rate-controlling membrane,” Current Opinion in Colloid and Interface Science. Elsevier Ltd, 17(3), hal. 156–165. doi: 10.1016/j.cocis.2012.02.001.

Cho, C. W., Choi, J. S., Yang, K. H., et al. (2009) “Enhanced transdermal absorption and pharmacokinetic evaluation of pranoprofen-ethylene-vinyl acetate matrix containing penetration enhancer in rats,” Archives of Pharmacal Research, 32(5), hal. 747–753. doi: 10.1007/s12272-009-1514-5.

Cho, C. W., Choi, J. S., Kim, S. J., et al. (2009) “Enhanced transdermal delivery of loratadine from the EVA matrix Transdermal delivery of loratadine from the EVA matrix,” Drug Delivery, 16(4), hal. 230–235. doi: 10.1080/10717540902872264.

Cho, C. W. et al. (2012) “Enhanced controlled transdermal delivery of ambroxol from the EVA matrix,” Indian Journal of Pharmaceutical Sciences, 74(2), hal. 127–132. doi: 10.4103/0250-474X.103844.

Cho, C. W., Choi, jun S. dan Shin, S. C. (2008) “Development of the ambroxol gels for enhanced transdermal delivery,” Drug Development and Industrial Pharmacy, 34(3), hal. 330–335. doi: 10.1080/03639040701662644.

Cho, C. W., Choi, J. S. dan Shin, S. C. (2009) “Enhanced transdermal controlled delivery of glimepiride from the ethylene-vinyl acetate matrix Enhanced transdermal delivery of glimepiride from the EVA matrix,” Drug Delivery, 16(6), hal. 320–330. doi: 10.1080/10717540903031084.

Choi, A. et al. (2008) “The effects of fatty acids in propylene glycol on the percutaneous absorption of alendronate across the excised hairless mouse skin,” International Journal of Pharmaceutics, 357(1–2), hal. 126–131. doi: 10.1016/j.ijpharm.2008.01.050.

Choi, J. et al. (2012) “Effect of fatty acids on the transdermal delivery of donepezil: In vitro and in vivo evaluation,” International Journal of Pharmaceutics. Elsevier B.V., 422(1–2), hal. 83–90. doi: 10.1016/j.ijpharm.2011.10.031.

Dubey, R. et al. (2009) “Ketorolac tromethamine transdermal gel: Development, in vitro and in vivo evaluation,” Journal of Pain and Palliative Care Pharmacotherapy, 23(1), hal. 26–34. doi: 10.1080/15360280902728062.

Harjoh, N., Wong, T. W. dan Caramella, C. (2020) “Transdermal insulin delivery with microwave and fatty acids as permeation enhancers,” International Journal of Pharmaceutics. Elsevier, 584(April), hal. 119416. doi: 10.1016/j.ijpharm.2020.119416.

Hashmat, D. et al. (2020) “Lornoxicam controlled release transdermal gel patch: Design, characterization and optimization using co-solvents as penetration enhancers,” PLoS ONE, 15(2), hal. 1–23. doi: 10.1371/journal.pone.0228908.

Heng, K. Y. et al. (2014) Handbook of Cosmeceutical Excipients and Their Safeties. Cambridge: Woodhead Publishing.

Ibrahim, S. A. dan Li, S. K., (2009) “Efficiency of Fatty Acids as Chemical Penetration Enhancers: Mechanisms

and Structure Enhancement Relationship,” Pharmaceutical Research, 27 (1), hal. 115-125. doi: 10.1007/s11095-009-9985-0.

Jiang, Y. et al. (2019) “Skin Delivery and Irritation Potential of Phenmetrazine as a Candidate Transdermal Formulation for Repurposed Indications,” AAPS Journal. The AAPS Journal, 21(4), hal. 1–9. doi: 10.1208/s12248-019-0335-9.

Jung, E. et al. (2013) “Effect of permeation enhancers on transdermal delivery of fluoxetine: In vitro and in vivo evaluation,” International Journal of Pharmaceutics. Elsevier B.V., 456(2), hal. 362–369. doi: 10.1016/j.ijpharm.2013.08.080.

Jung, S. Y. et al. (2009) “Formulation and evaluation of ubidecarenone transdermal delivery systems Ubidecarenone transdermal delivery systems,” Drug Development and Industrial Pharmacy, 35(9), hal. 1029–1034. doi: 10.1080/03639040902755205.

Kandimalla, K. et al. (1999) “Effect of Fatty acids on the Permeation of Melatonin across Rat and Pig Skin In-vitro and on the Transepidermal Water Loss in Rats In-vivo,” Journal of Pharmacy and Pharmacology, 51(7), hal. 783–790. doi: 10.1211/0022357991773140.

Karakatsani, M., Dedhiya, M. dan Plakogiannis, F. M. (2010) “The effect of permeation enhancers on the viscosity and the release profile of transdermal hydroxypropyl methylcellulose gel formulations containing diltiazem HCl,” Drug Development and Industrial Pharmacy, 36(10), hal. 1195–1206. doi: 10.3109/03639041003695105.

Kaur, D. dan Singh, R. (2015) “A Novel Approach: Transdermal Gel,” International Journal of Pharma Research & Review, 4(10), hal. 41–50.

Kezutyte, T. et al. (2013) “Studying the penetration of fatty acids into human skin by ex vivo TOF-SIMS imaging,” Biointerphases, 8(1), hal. 1–8. doi: 10.1186/1559-4106-8-3.

Kim, M. J. et al. (2008) “Skin permeation enhancement of diclofenac by fatty acids,” Drug Delivery, 15(6), hal. 373–379. doi: 10.1080/10717540802006898.

Maurya, A. dan Murthy, S. N. (2014) “Pretreatment with skin permeability enhancers: Importance of duration and composition on the delivery of diclofenac sodium,” Journal of Pharmaceutical Sciences, 103(5), hal. 1497–1503. doi: 10.1002/jps.23938.

Mittal, A. et al. (2008) “The effect of penetration enhancers on permeation kinetics of nitrendipine in two different skin models,” Biological and Pharmaceutical Bulletin, 31(9), hal. 1766–1772. doi: 10.1248/bpb.31.1766.

Moreira, T. S. A., De Sousa, V. P. dan Pierre, M. B. R. (2010) “A novel transdermal delivery system for the anti-inflammatory lumiracoxib: Influence of oleic acid on in vitro percutaneous absorption and in vivo potential cutaneous irritation,” AAPS PharmSciTech, 11(2), hal. 621–629. doi: 10.1208/s12249-010-9420-1.

Nair, A., Reddy, C. dan Jacob, S. (2009) “Delivery of a classical antihypertensive agent through the skin by chemical enhancers and iontophoresis,” Skin Research and Technology, 15(2), hal. 187–194. doi: 10.1111/j.1600-0846.2009.00350.x.

Patel, R. P., Gaiakwad, D. R. dan Patel, N. A. (2014) “Formulation, optimization, and evaluation of a transdermal patch of heparin sodium,” Drug discoveries & therapeutics, 8(4), hal. 185–193. doi: 10.5582/ddt.2014.01030.

Puri, A. et al. (2017) “Effects of chemical and physical enhancement techniques on transdermal delivery of 3-fluoroamphetamine hydrochloride,” International Journal of Pharmaceutics. Elsevier B.V., 528(1–2), hal. 452–462. doi: 10.1016/j.ijpharm.2017.06.041.

Ravula, R. et al. (2016) “Formulation optimization of a drug in adhesive transdermal analgesic patch,” Drug Development and Industrial Pharmacy. Taylor & Francis, 42(6), hal. 862–870. doi: 10.3109/03639045.2015.1071832.

Ren, C. et al. (2008) “Effect of permeation enhancers and organic acids on the skin permeation of indapamide,” International Journal of Pharmaceutics, 350(1–2), hal. 43–47. doi: 10.1016/j.ijpharm.2007.08.020.

Del Rio-Sancho, S. et al. (2012) “Transdermal absorption of memantine - Effect of chemical enhancers, iontophoresis, and role of enhancer lipophilicity,” European Journal of Pharmaceutics and Biopharmaceutics. Elsevier B.V., 82(1), hal. 164–170. doi: 10.1016/j.ejpb.2012.06.005.

Ruela, A. L. M. et al. (2016) “Evaluation of skin absorption of drugs from topical and transdermal formulations,” Brazilian Journal of Pharmaceutical Sciences, 52(3), hal. 527–544.

Schroeder, I. Z. et al. (2007) “Delivery of ethinylestradiol from film forming polymeric solutions across human epidermis in vitro and in vivo in pigs,” Journal of Controlled Release, 118(2), hal. 196–203. doi: 10.1016/j.jconrel.2006.12.013.

Shin, S. C. et al. (2007) “Development and biopharmaceutical evaluation of quinupramine-EVA matrix containing penetration enhancer for the enhanced transdermal absorption in rats,” Pharmaceutical Development and Technology, 12(5), hal. 429–436. doi: 10.1080/10837450701555695.

Singh Malik, D., Mital, N. dan Kaur, G. (2016) “Topical drug delivery systems: A patent review,” Expert Opinion on Therapeutic Patents, 26(2), hal. 213–228. doi: 10.1517/13543776.2016.1131267.

Smith, E. W. dan Maibach, H. I. (2006) Percutaneous Penetration Enhancers. 2nd Editio. Boca Raton: CRC Press. doi: 10.4324/9781315573007-1.

Thakur, R. A., Michniak, B. B. dan Meidan, V. M. (2007) “Transdermal and buccal delivery of methylxanthines through human tissue in vitro,” Drug Development and Industrial Pharmacy, 33(5), hal. 513–521. doi: 10.1080/03639040600901994.

Ueda, C. T. et al. (2009) “Topical and Transdermal Drug Products,” Pharmacopeial Forum, 35, hal. 750–764. doi: 10.1787/9789264071087-pt.

Wang, M. Y., Yang, Y. Y. dan Heng, P. W. S. (2005) “Skin permeation of physostigmine from fatty acids-based formulations: Evaluating the choice of solvent,” International Journal of Pharmaceutics, 290(1–2), hal. 25–36. doi: 10.1016/j.ijpharm.2004.10.027.

Williams, A. C. dan Barry, B. W. (2012) “Penetration enhancers,” Advanced Drug Delivery Reviews. Elsevier B.V., 64(SUPPL.), hal. 128–137. doi: 10.1016/j.addr.2012.09.032.

Yamato, K. et al. (2009) “Effect of penetration enhancers on transdermal delivery of propofol,” Biological and Pharmaceutical Bulletin, 32(4), hal. 677–683. doi: 10.1248/bpb.32.677.

Yang, Y., Kalluri, H. dan Banga, A. K. (2011) “Effects of chemical and physical enhancement techniques on transdermal delivery of cyanocobalamin (vitamin B12) in vitro,” Pharmaceutics, 3(3), hal. 474–484. doi: 10.3390/pharmaceutics3030474.


Full Text: PDF

DOI: 10.15408/pbsj.v3i1.18448

Refbacks

  • There are currently no refbacks.