Ex-vivo skin permeation studies of sumatriptan succinate using different solvent systems and its comparison with PLGA nanoparticles
Abstract
Sumatripatan succinate (SS) is a 5-HT1D agonist used in migraine therapy. Its low oral bioavailability (~15 %) is due to extensive pre-systemic metabolism and low biological half-life. The frequent administration of SS is required to maintain effective plasma concentration. In the present investigation, polymeric nanoparticles of SS (SS-NPs) were prepared by W1/O/W2 double emulsion solvent evaporation method followed by probe sonication. Poly-(lactide-co-glycolide) (PLGA) and poloxamer 188 were used as polymer and surfactant respectively to formulate SS-NPs. The particle size, polydispersity index, zeta potential, percent entrapment efficiency of SS-NPs were found to be 126 nm, 0.06, (-) 24.1 mV, 32.52 ± 2.34 % respectively. Characterization of lyophilized SS-NPs revealed formation of drug entrapped amorphous SS-NPs. Ex-vivo skin permeation studies of SS were conducted using distilled water, ethanol (EtOH), propylene glycol (PG) and their binary combinations. The lag time, flux, permeability and steady state permeability coefficient and enhancement ratio were determined. The ex-vivo permeation profiles of SS in different solvent systems were compared with SS-NPs in distilled water. The maximum flux of 345.8 µg.cm-2.h-1 was obtained with solvent system comprising 33% PG in EtOH. The minimum lag time and a comparable flux value was obtained in ex-vivo diffusion studies of SS-NPs. Hence, it can be concluded that SS-NPs can be administered in transdermal drug delivery system using a solvent system comprising 33%PG in EtOH. The present investigation indicated that using suitable solvent system and PLGA nanoparticles, the skin permeation of SS can be enhanced.
Keywords: Migraine, sumatriptan succinate, poly-(lactide-co-glycolide), nanoparticles, transdermal patch
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References
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2. Villalón CM, Centurión D, Valdivia LF, de Vries P, Saxena PR. Migraine: Pathophysiology, pharmacology, treatment and future trends. Curr. Vasc. Pharmacol. 2003; 1(1):71-84.
3. Ebell MH. Diagnosis of migraine headache. Am. Fam. Physician. 2006; 74(12):2087-2088.
4. Weitzel KW, Thomas ML, Small RE. Migraine: A comprehensive review of new treatment options. Pharmacotherapy. 1999; 19(8):957–973.
5. Diamond S, Bigal ME, Silberstein S. Patterns of diagnosis and acute and preventive treatment for migraine in the United States: Results from the American Migraine Prevalence and Prevention study. Headache. 2007; 47(3):355–363.
6. Jagdale SC, Pawar CR. Application of design of experiment for polyox and xanthan gum coated floating pulsatile delivery of sumatriptan succinate in migraine treatment, Biomed. Res. Int. 2014; 547212.
7. Hilaire ML, Cross LB, Eichner SF. Treatment of migraine headaches with sumatriptan in pregnancy, Ann. Pharmacother. 2004; (38):1726–1730.
8. Kolev P. Migraine: principles of acute treatment and prevention, Eur. Neuropsychopharmacol. (2007); 17S:134.
9. Levy D, Jakubowski M, Burstein R. Disruption of communication between peripheral and central trigeminovascular neurons mediates the antimigraine action of 5HT 1B/1D receptor agonists, Proc. Natl. Acad. Sci. U. S. A. 2004; 101:4274–4279.
10. Silberstein SD. Practice parameter: evidence based guidelines for migraine headache (an evidence-based review), Neurology, 2000; 55:754–763.
11. Tfelt-Hansen PC. Does sumatriptan cross the blood–brain barrier in animals and man? J. Headache Pain.2010; 11:5–12.
12. Kreuter J. Nanoparticulate systems for brain delivery of drugs, Adv. Drug Deliv. Rev. 2001; 47:65–81.
13. Kreuter J. Transport of drugs across the blood–brain barrier by nanoparticles, Curr. Med. Chem. Cent. Nerv. Syst. Agents. 2 (2002); 241–249.
14. Abbott NJ. Evidence for bulk flow of brain interstitial fluid: significance for physiology and pathology. Neurochem. Int. (2004); 45:545–552.
15. Abbott NJ, Patabendige AA, Dolman DE, Yusof SR, Begley DJ. Structure and function of the blood–brain barrier. Neurobiol. Dis. 2010; 37:13–25.
16. Candela P, Gosselet F, Saint-Pol J, Apical-to-basolateral transport of amyloid-β peptides through blood–brain barrier cells is mediated by the receptor for advanced glycation end-products and is restricted by P-glycoprotein. J. Alzheimers Dis. 2010; 22:849–859.
17. Piergiorgio Gentile, Valeria Chiono, Irene Carmagnola, and Paul V. Hatton An Overview of Poly(lactic-co-glycolic) Acid (PLGA)-Based Biomaterials for Bone Tissue Engineering. Int. J. Mol. Sci. 2014; 15(3): 3640–3659.
18. Gao X, Qian J, Zheng S, Changyi Y, Zhang J, Ju S, Overcoming the blood–brain barrier for delivering drugs into the brain by using adenosine receptor nanoagonist. ACS Nano. 2014; 8:3678-3689.
19. Choi CHJ, Alabi CA, Webster P, Davis M.E. Mechanism of active targeting in solid tumors with transferrin-containing gold nanoparticle Proc. Natl. Acad. Sci. U. S. A. 2010; 107:1235-1240.
20. Deepti Mittal, Shadab Md, Quamrul Hasan, Mohammad Fazil, Asgar Ali, Sanjula Baboota, and Javed Ali. Brain targeted nanoparticulate drug delivery system of rasagiline via intranasal route. Drug Delivery. 2016; 23(1):130-139.
21. Wissing SA, Muller RH. Structural characterization of Q10-loaded solid lipid nanoparticles. Pharm. Res. 2004; 21:400-405.
22. Asasutjarit R, Lorenzen SI, Sirivichayakul S, Ruxrungtham K, Ruktanonchai U, Ritthidej GC. Effect of solid lipid nanoparticles formulation compositions on their size, zeta potential and potential for in-vitro pHIS-HIV-Hugag transfection. Pharm. Res. 2007; 24:1098-1107.
23. Sharma G, Jasuja ND, Kumar, Ali MI. Biological synthesis of silver nanoparticles by cell-free extract of spirulina plantesis. J. Nanotech. 2015; 1-6.
24. Shu-Ben Sun, Ping Liu, Fa-Ming Shao, and Qi-Long Miao. Formulation and evaluation of PLGA nanoparticles loaded capecitabine for prostate cancer. Int. J. Clin. Exp. Med. 2015; 8(10):19670–19681.
25. Adeyinka Aina, Manish Gupta, Nashiru Bill, Stephen Doughty. Monitoring model drug microencapsulation in PLGA scaffolds using X-ray powder diffraction Saudi Pharmaceutical Journal, March 2016; 24 (2):227-231.
26. Gungor S, Bektas A, Alp FI. Matrix-type transdermal patches of verapamil hydrochloride: in-vitro permeation studies through excised rat skin and pharmacodynamic evaluation in rats. Pharm. Dev. Technol., 2008; 4:283-289.
27. Xi H, Yang Y, Zhao D. Transdermal patches for site-specific delivery of anastrozole: in-vitro and local tissue disposition evaluation Int. J Pharm., 2010; (1–2):73-78.
28. Rhee YS, Nguyen T, Park ES, Chi, SC. Formulation and biopharmaceutical evaluation of a transdermal patch containing aceclofenac. Arch. Pharm. Res., (2013); 5:602-607.
29. Aggarwal G, Dhawan S, Hari Kumar SL. Formulation, in-vitro and in-vivo evaluation of transdermal patches containing risperidone Drug Dev. Ind. Pharm. 2013; 1:39-50.
30. Amnuaikit C, Ikeuchi I, Ogawara K, Higaki K, Kimura T. Skin permeation of propranolol from polymeric film containing terpene enhancers for transdermal use. Int. J. Pharm., 2005; (1–2):167-178.
31. Arora P, Mukherjee B. Design, development, physicochemical, and in vitro and in vivo evaluation of transdermal patches containing diclofenac diethylammonium salt. J. Pharm. Sci., 2002; 9:2076-2089.
32. Mamatha T, Venkateswara Rao J, Mukkanti K, Ramesh G. Development of matrix type transdermal patches of lercanidipine hydrochloride: physicochemical and in-vitro characterization. DARU J. Pharm. Sci., 2010; 18(1):9-16.
33. Panchagnula R, Salve PS, Thomas NS, Jain AK, Ramarao P. Transdermal delivery of naloxone: effect of water, propylene glycol, ethanol and their binary combinations on permeation through rat skin. Int. J. Pharm. 2001; May 21; 219(1-2):95-105.
34. Ostertag F, Weiss J, McClements DJ. Low-energy formation of edible nanoemulsions: factors influencing droplet size produced by emulsion phase inversion. J. Colloid Interface Sci. 2012; 388(1):95-102.
35. Upadhyay S, Patel J, Patel V, Saluja A. Effect of different lipids and surfactants on formulation of solid lipid nanoparticles incorporating tamoxifen citrate. J. Pharm. Bioallied Sci. 2012; 4(Suppl.1): S112-S113.
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Salve PS, Gupta RR. Ex-vivo skin permeation studies of sumatriptan succinate using different solvent systems and its comparison with PLGA nanoparticles. JDDT [Internet]. 15Aug.2019 [cited 19May2024];9(4-s):59-7. Available from: https://jddtonline.info/index.php/jddt/article/view/3247
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