Using Microemulsion as Carrier for Drug Transdermal Delivery: The Effect of Surfactants and Cosurfactants

Author(s): I-Ju Lu, Yaw-Syan Fu, Wen-Yu Chang, Pao-Chu Wu*

Journal Name: Current Pharmaceutical Design

Volume 25 , Issue 10 , 2019


Become EABM
Become Reviewer
Call for Editor

Abstract:

Background: The purpose of this study was to evaluate the effect of types of surfactants and cosurfactants on physicochemical properties and permeability of sumatriptan-loaded microemulsions through rat skin.

Methods: Different types of surfactants and cosurfactants were used to prepare drug-loaded microemulsions. The physicochemical characters and permeability parameters of these formulations were measured.

Results: The experimental microemulsions with varying components had small droplet size ranging from 24.6 nm to 2568.8 nm, low viscosity ranging from 7.49 to 43.34 cps and significant permeation enhancement ratio ranging from 23.0 to 98.6 when compared to the control group.

Conclusion: The composition and proportion of surfactants and cosurfactants were key factors for the physiochemical properties of drug-loaded microemulsions. The cumulative transdermal amount of the microemulsion containing mixture surfactant of Laureth-3/Laureth-23 was higher than that of the microemulsion with a mixture of Tween 80/Span 20. In the selected cosurfactant, diethylene glycol monoethyl ether (DEGMEE) showed highest permeation enhancement. Thermodynamic stability tests revealed that the experimental microemulsion was a stable enough formulation to be considered as a suitable carrier for sumatriptan.

Keywords: Sumatriptan, microemulsion, surfactants, cosurfactants, thermodynamic stability, Laureth-3/Laureth-23.

[1]
Femenía-Font A, Padula C, Marra F, et al. Bioadhesive monolayer film for the in vitro transdermal delivery of sumatriptan. J Pharm Sci 2006; 95(7): 1561-9.
[http://dx.doi.org/10.1002/jps.20638] [PMID: 16721755]
[2]
Balaguer-Fernández C, Padula C, Femenía-Font A, Merino V, Santi P, López-Castellano A. Development and evaluation of occlusive systems employing polyvinyl alcohol for transdermal delivery of sumatriptan succinate. Drug Deliv 2010; 17(2): 83-91.
[http://dx.doi.org/10.3109/10717540903509019] [PMID: 20067437]
[3]
Calatayud-Pascual MA, Balaguer-Fernández C, Serna-Jiménez CE, et al. Effect of iontophoresis on in vitro transdermal absorption of almotriptan. Int J Pharm 2011; 416(1): 189-94.
[http://dx.doi.org/10.1016/j.ijpharm.2011.06.039] [PMID: 21736929]
[4]
Ito Y, Yoshimura M, Tanaka T, Takada K. Effect of lipophilicity on the bioavailability of drugs after percutaneous administration by dissolving microneedles. J Pharm Sci 2012; 101(3): 1145-56.
[http://dx.doi.org/10.1002/jps.22814] [PMID: 22086760]
[5]
Amjadi M, Mostaghaci B, Sitti M. Recent Advances in Skin Penetration Enhancers for Transdermal Gene and Drug Delivery. Curr Gene Ther 2017; 17(2): 139-46.
[http://dx.doi.org/10.2174/1566523217666170510151540] [PMID: 28494734]
[6]
Balaguer-Fernández C, Femenía-Font A, Merino V, et al. Elastic vesicles of sumatriptan succinate for transdermal administration: characterization and in vitro permeation studies. J Liposome Res 2011; 21(1): 55-9.
[http://dx.doi.org/10.3109/08982101003736002] [PMID: 20429812]
[7]
Lim DJ, Vines JB, Park H, Lee SH. Microneedles: a versatile strategy for transdermal delivery of biological molecules. Int J Biol Macromol 2017. S0141-8130: 33217-8.
[8]
Malinovskaja-Gomez K, Espuelas S, Garrido MJ, Hirvonen J, Laaksonen T. Comparison of liposomal drug formulations for transdermal iontophoretic drug delivery. Eur J Pharm Sci 2017; 106: 294-301.
[http://dx.doi.org/10.1016/j.ejps.2017.06.025] [PMID: 28625748]
[9]
Gupta R, Rai B. In-silico design of nanoparticles for transdermal drug delivery application. Nanoscale 2018; 10(10): 4940-51.
[http://dx.doi.org/10.1039/C7NR07898F] [PMID: 29485168]
[10]
Lin H, Xie Q, Huang X, et al. Increased skin permeation efficiency of imperatorin via charged ultradeformable lipid vesicles for transdermal delivery. Int J Nanomedicine 2018; 13: 831-42.
[http://dx.doi.org/10.2147/IJN.S150086] [PMID: 29467573]
[11]
Mahmood S, Mandal UK, Chatterjee B. Transdermal delivery of raloxifene HCl via ethosomal system: Formulation, advanced characterizations and pharmacokinetic evaluation. Int J Pharm 2018; 542(1-2): 36-46.
[http://dx.doi.org/10.1016/j.ijpharm.2018.02.044] [PMID: 29501737]
[12]
Moyano-Mendez JR, Fabbrocini G, De Stefano D, et al. Enhanced antioxidant effect of trans-resveratrol: potential of binary systems with polyethylene glycol and cyclodextrin. Drug Dev Ind Pharm 2014; 40(10): 1300-7.
[http://dx.doi.org/10.3109/03639045.2013.817416] [PMID: 23862976]
[13]
Pandita D, Kumar S, Poonia N, Lather V. Solid lipid nanoparticles enhance oral bioavailability of resveratrol, a natural polyphenol. Food Res Int 2014; 62: 1165-74.
[http://dx.doi.org/10.1016/j.foodres.2014.05.059]
[14]
Danafar H. Applications of Copolymeric Nanoparticles in Drug Delivery Systems. Drug Res (Stuttg) 2016; 66(10): 506-19.
[http://dx.doi.org/10.1055/s-0042-109865] [PMID: 27403578]
[15]
Danafar H, Manjili HK, Najafi M. Study of Copolymer Composition on Drug Loading Efficiency of Enalapril in Polymersomes and Cytotoxicity of Drug Loaded Nanoparticles. Drug Res (Stuttg) 2016; 66(9): 495-504.
[http://dx.doi.org/10.1055/s-0042-110931] [PMID: 27434113]
[16]
Gharebaghi F, Dalali N, Ahmadi E, Danafar H. Preparation of wormlike polymeric nanoparticles coated with silica for delivery of methotrexate and evaluation of anticancer activity against MCF7 cells. J Biomater Appl 2017; 31(9): 1305-16.
[http://dx.doi.org/10.1177/0885328217698063] [PMID: 28447548]
[17]
Park SN, Jo N, Jeon SH. Chitosan-coated liposomes for enhanced skin permeation of resveratrol. J Ind Eng Chem 2014; 20: 1481-5.
[http://dx.doi.org/10.1016/j.jiec.2013.07.035]
[18]
Scognamiglio I, De Stefano D, Campani V, et al. Nanocarriers for topical administration of resveratrol: a comparative study. Int J Pharm 2013; 440(2): 179-87.
[http://dx.doi.org/10.1016/j.ijpharm.2012.08.009] [PMID: 22909994]
[19]
Zillich OV, Schweiggert-Weisz U, Hasenkopf K, Eisner P, Kerscher M. Release and in vitro skin permeation of polyphenols from cosmetic emulsions. Int J Cosmet Sci 2013; 35(5): 491-501.
[http://dx.doi.org/10.1111/ics.12072] [PMID: 23763665]
[20]
Baboota S, Shakeel F, Ahuja A, Ali J, Shafiq S. Design, development and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxib. Acta Pharm 2007; 57(3): 315-32.
[http://dx.doi.org/10.2478/v10007-007-0025-5] [PMID: 17878111]
[21]
Chen H, Chang X, Weng T, et al. A study of microemulsion systems for transdermal delivery of triptolide. J Control Release 2004; 98(3): 427-36.
[http://dx.doi.org/10.1016/j.jconrel.2004.06.001] [PMID: 15312998]
[22]
Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev 2000; 45(1): 89-121.
[http://dx.doi.org/10.1016/S0169-409X(00)00103-4] [PMID: 11104900]
[23]
Lin YH, Tsai MJ, Fang YP, Fu YS, Huang YB, Wu PC. Microemulsion formulation design and evaluation for hydrophobic compound: Catechin topical application. Colloids Surf B Biointerfaces 2018; 161: 121-8.
[http://dx.doi.org/10.1016/j.colsurfb.2017.10.015] [PMID: 29055864]
[24]
Jhee SS, Shiovitz T, Crawford AW, Cutler NR. Pharmacokinetics and pharmacodynamics of the triptan antimigraine agents: a comparative review. Clin Pharmacokinet 2001; 40(3): 189-205.
[http://dx.doi.org/10.2165/00003088-200140030-00004] [PMID: 11327198]
[25]
Tfelt-Hansen P, De Vries P, Saxena PR. Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs 2000; 60(6): 1259-87.
[http://dx.doi.org/10.2165/00003495-200060060-00003] [PMID: 11152011]
[26]
Femenía-Font A, Balaguer-Fernández C, Merino V, López-Castellano A. Combination strategies for enhancing transdermal absorption of sumatriptan through skin. Int J Pharm 2006; 323(1-2): 125-30.
[http://dx.doi.org/10.1016/j.ijpharm.2006.05.049] [PMID: 16809010]
[27]
Ito Y, Kashiwara S, Fukushima K, Takada K. Two-layered dissolving microneedles for percutaneous delivery of sumatriptan in rats. Drug Dev Ind Pharm 2011; 37(12): 1387-93.
[http://dx.doi.org/10.3109/03639045.2011.576426] [PMID: 21545233]
[28]
Femenía-Font A, Merino V, Rodilla V, López-Castellano A. High-performance liquid chromatographic determination of sumatriptan after in vitro transdermal diffusion studies. J Pharm Biomed Anal 2005; 37(3): 621-6.
[http://dx.doi.org/10.1016/j.jpba.2004.11.029] [PMID: 15740926]
[29]
Ge Z, Tessier E, Neirinck L, Zhu Z. High performance liquid chromatographic method for the determination of sumatriptan with fluorescence detection in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci 2004; 806(2): 299-303.
[http://dx.doi.org/10.1016/j.jchromb.2004.03.057] [PMID: 15171943]
[30]
Azeem A, Talegaonkar S, Negi LM, Ahmad FJ, Khar RK, Iqbal Z. Oil based nanocarrier system for transdermal delivery of ropinirole: a mechanistic, pharmacokinetic and biochemical investigation. Int J Pharm 2012; 422(1-2): 436-44.
[http://dx.doi.org/10.1016/j.ijpharm.2011.10.039] [PMID: 22057087]
[31]
Zidan AS, Kamal N, Alayoubi A, et al. Effect of isopropyl myristate on transdermal oermeation of testosterone from carbopol gel. J Pharm Sci 2017; 106(7): 1805-13.
[http://dx.doi.org/10.1016/j.xphs.2017.03.016] [PMID: 28341597]
[32]
Said M, Elsayed I, Aboelwafa AA, Elshafeey AH. Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability. Drug Deliv 2017; 24(1): 1159-69.
[http://dx.doi.org/10.1080/10717544.2017.1365392] [PMID: 28831842]
[33]
Silva AE, Barratt G, Chéron M, Egito ES. Development of oil-in-water microemulsions for the oral delivery of amphotericin B. Int J Pharm 2013; 454(2): 641-8.
[http://dx.doi.org/10.1016/j.ijpharm.2013.05.044] [PMID: 23726904]
[34]
Shigemoto N, Al-Maamari RS, Jibril BY, Hirayama A, Sueyoshi M. Effect of Water Content and Surfactant Type on Viscosity and Stability of Emulsified Heavy Mukhaizna Crude Oil. Energy Fuels 2007; 21: 1014-8.
[http://dx.doi.org/10.1021/ef060259o]
[35]
Sripriya R, Muthu Raja K, Santhosh G, Chandrasekaran M, Noel M. The effect of structure of oil phase, surfactant and co-surfactant on the physicochemical and electrochemical properties of bicontinuous microemulsion. J Colloid Interface Sci 2007; 314(2): 712-7.
[http://dx.doi.org/10.1016/j.jcis.2007.05.080] [PMID: 17585927]
[36]
Shinde UA, Modani SH, Singh KH. Design and development of repaglinide microemulsion gel for transdermal delivery. AAPS PharmSciTech 2017; 19(1): 315-25.
[http://dx.doi.org/doi:10.1208/s12249-017-0811-4] [PMID: 28717973]
[37]
Peltola S, Saarinen-Savolainen P, Kiesvaara J, Suhonen TM, Urtti A. Microemulsions for topical delivery of estradiol. Int J Pharm 2003; 254(2): 99-107.
[http://dx.doi.org/10.1016/S0378-5173(02)00632-4] [PMID: 12623186]
[38]
Shokri J, Nokhodchi A, Dashbolaghi A, Hassan-Zadeh D, Ghafourian T, Barzegar Jalali M. The effect of surfactants on the skin penetration of diazepam. Int J Pharm 2001; 228(1-2): 99-107.
[http://dx.doi.org/10.1016/S0378-5173(01)00805-5] [PMID: 11576772]
[39]
Qumbar M. Ameeduzzafar, Imam SS, Ali J, Ahmad J, Ali A. Formulation and optimization of lacidipine loaded niosomal gel for transdermal delivery: In-vitro characterization and in-vivo activity. Biomed Pharmacother 2017; 93: 255-66.
[http://dx.doi.org/10.1016/j.biopha.2017.06.043] [PMID: 28738502]
[40]
Birdi KS. Microemulsions: Effect of alkyl chain length of alcohol and alkane. Colloid Polym Sci 1982; 260: 628-31.
[http://dx.doi.org/10.1007/BF01422596]
[41]
El Maghraby GM. Transdermal delivery of hydrocortisone from eucalyptus oil microemulsion: effects of cosurfactants. Int J Pharm 2008; 355(1-2): 285-92.
[http://dx.doi.org/10.1016/j.ijpharm.2007.12.022] [PMID: 18243604]
[42]
Ameen D, Michniak-Kohn B. Transdermal delivery of dimethyl fumarate for Alzheimer’s disease: Effect of penetration enhancers. Int J Pharm 2017; 529(1-2): 465-73.
[http://dx.doi.org/10.1016/j.ijpharm.2017.07.031] [PMID: 28709939]
[43]
Moosavi-Movahedi AA, Safarian S, Hakimelahi GH, et al. QSAR analysis for ADA upon interaction with a series of adenine derivatives as inhibitors. Nucleosides Nucleotides Nucleic Acids 2004; 23(3): 613-24.
[http://dx.doi.org/10.1081/NCN-120030719] [PMID: 15113027]
[44]
Al Azzam KM, Saad B, Tat CY, Mat I, Aboul-Enein HY. Stability-indicating micellar electrokinetic chromatography method for the analysis of sumatriptan succinate in pharmaceutical formulations. J Pharm Biomed Anal 2011; 56(5): 937-43.
[http://dx.doi.org/10.1016/j.jpba.2011.08.007] [PMID: 21873014]
[45]
Chamani J, Heshmati M. Mechanism for stabilization of the molten globule state of papain by sodium n-alkyl sulfates: spectroscopic and calorimetric approaches. J Colloid Interface Sci 2008; 322(1): 119-27.
[http://dx.doi.org/10.1016/j.jcis.2008.03.001] [PMID: 18405913]


Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 25
ISSUE: 10
Year: 2019
Published on: 04 August, 2019
Page: [1052 - 1058]
Pages: 7
DOI: 10.2174/1381612825666190527091528
Price: $65

Article Metrics

PDF: 24
HTML: 6
EPUB: 1