EFFECT OF MENTHOL ON THE TRANSDERMAL PERMEATION OF ACECLOFENAC FROM MICROEMULSION FORMULATION

Authors

  • Abdul Baquee Ahmed Department of Pharmaceutics, Girijananda Chowdhury Institute of Pharmaceutical Science, Hathkhowapara, Azara, Guwahati, Assam 781017
  • Gouranga Das Girijananda Chowdhury Institute of Pharmaceutical Science, Hathkhowapara, Azara, Guwahati, Assam 781017

DOI:

https://doi.org/10.22159/ijap.2019v11i2.30988

Keywords:

Menthol, Microemulsion, Transdermal flux, Surfactant, Co-surfactant

Abstract

Objective: The aim of this investigation was to enhance the transdermal permeation of aceclofenac (ACF) from microemulsion formulation using menthol as a natural permeation enhancer.

Methods: Microemulsion containing 2% w/v of ACF was prepared by a titration method with different concentration of oil, surfactant and co-surfactant. The prepared microemulsion was evaluated for droplet size, viscosity, pH and in vitro skin permeation studies. Menthol at 3-8% w/w was added to the selected microemulsion formulation and their effect on skin permeation was evaluated across rat epidermis using modified Keshary-Chien diffusion cell. The Fourier transform infrared spectroscopy (FT-IR) was performed to understand the regulation action of menthol in the skin permeability barrier.

Results: The average droplet size of the microemulsion was found to be 89.4±2.12 to 175.2±3.10 nm. The transdermal flux of the microemulsion containing 8% w/w menthol showed 2.9 fold increases in transdermal flux of ACF compared with the formulation without menthol. Result of FT-IR studies showed decrease in peak height of the symmetric and asymmetric C-H stretching vibrations may be because of the extraction of the stratum corneum (SC) lipids and the alteration of the skin permeability barrier.

Conclusion: This result suggests that menthol significantly enhanced the transdermal permeation of ACF and may be an effective natural penetration enhancer for transdermal delivery of the drug.

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Author Biography

Abdul Baquee Ahmed, Department of Pharmaceutics, Girijananda Chowdhury Institute of Pharmaceutical Science, Hathkhowapara, Azara, Guwahati, Assam 781017

Pharmaceutical Sciences

HOD, Department of Pharmaceutics

References

Brogden RN, Wiseman LR. Aceclofenac: a review of its pharmacodynamic properties and therapeutic potential in the treatment of rheumatic disorders and in pain management. Drugs 1996;52:113-24.

Jeeboi L, Boddu S. UV spectrophotometric method for simultaneous estimation of tramadol hydrochloride and aceclofenac in bulk and tablet dosage form. Int J Pharm Pharm Sci 2016;8:334-40.

Alvarez Larena A, Piniella JF, Carrasco E. Crystal structure and spectroscopic study of 2-[(2, 6-dichlorophenyl) amino] phenylacetoxyacetic acid (aceclofenac). J Chem Crystallography 1992;22:323–8.

McNeill SC, Potts RO, Francoeur ML. Local enhanced topical delivery (LETD) of drugs. Pharm Res 1992;9:1422-7.

Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Delivery Rev 2002;54(Suppl 1):S77–98.

Chaiyana W, Phongpradist R, Leelapornpisid P, Anuchapreeda S. Microemulsion-based hydrogel for topical delivery of indomethacin. Int J Pharm Pharm Sci 2015;7:213-9.

Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Delivery Rev 2000;45:89–121.

Gasco MR. Microemulsions in the pharmaceutical field. In: Persperctives and Applications, Industrial Applications of Microemulsions. 1st ed. Marcel Dekker Inc.: New York; 1997; 45:97–122.

Zhong D, Mo F, Li S, Yuan Y. Investigation of microemulsion system for transdermal delivery of Meloxicam. Int J Pharm 2006;321:117–23.

Peltola S, Savolainen PS, Kiesvaara J, Suhonen TM, Urtti A. Microemulsions for topical delivery of estradiol. Int J Pharm 2003;254:99–107.

Chen HB, Chang XL, Weng T, Zhao XZ, Gao ZH, Yang YJ, et al. A study of microemulsion systems for transdermal delivery of triptolide. J Controlled Release 2004;98:427–36.

Wiechers JW. The barrier functions of the skin in relation to percutaneous absorption of drugs. Pharm Weekbl Sci 1989;11:185-98.

Krishnaiah YSR, Bhaskar P, Satyanarayana V. Penetration-enhancing effect of ethanol-water solvent system and an ethanolic solution of carvone on transdermal permeability of nimodipine from HPMC gel across rat abdominal skin. Pharm Dev Technol 2004;9:63–74.

Pfister W, Dean S, Hsieh S. Permeation enhancers compatible with transdermal drug delivery systems. I. Selection and formulation considerations. Pharm Technol 1990;8:132–40.

Gao S, Singh J. In vitro percutaneous absorption enhancement of lipophilic drug tamoxifen by terpenes. J Controlled Release 1998;51:193–9.

Hori M, Satoch H, Miabach HI, Guy RH. Enhancement effect of propranolol hydrochloride and diazepam skin absorption in vitro: effect of enhancer lipophilicity. J Pharm Sci 1991;80:32–5.

Okabe H, Takayama K, Ogura A, Nagai T. Effects of limonene and related compounds on the percutaneous absorption of indomethacin. Drug Des Delivery 1989;4:313–21.

Djordjevic L, Primorac M, Stupar M, Krajisnik D. Characterization of caprylocaproyl macrogolglycerides based microemulsion drug delivery vehicles for an amphiphilic drug. Int J Pharm 2004;271:11–9.

Thomas NS, Panchagnula R. Transdermal delivery of zidovudine: effect of vehicles on permeation across rat skin. Eur J Pharm Sci 2003;18:71-3.

Krishnaiah YSR, Satyanarayana V, Bhaskar P. Enhanced percutaneous permeability of nicardipine hydrochloride by carvone across the rat abdominal skin. Drug Dev Ind Pharm 2003;29:191–202.

Bhatia KS, Gao S, Singh J. Effect of penetration enhancers and iontophoresis on FT-IR spectroscopy and LHRH permeability through porcine skin. J Controlled Release 1997;47:81–9.

Casal HL, Mantsch HH. Polymeric phase behavior of phospolipid membranes studied by infrared spectroscopy. Biochim Biophys Acta 1984;779:381–401.

Krishnaiah YSR, Bhaskar P, Satyanarayana V. Penetration-enhancing effect of ethanol-water solvent system and an ethanolic solution of carvone on transdermal permeability of nimodipine from HPMC gel across rat abdominal skin. Pharm Dev Technol 2004;9:63–74.

Higuchi T. Physical analysis of percutaneous absorption processes from creams and ointments. J Soc Cosmet Chem 1960;11:85–97.

Thacharodi D, Rao KP. Transdermal absorption of nifedipine from microemulsions of lipophilic skin penetration enhancers. Int J Pharm 1994;111:235–41.

Alvarez Figueroa MJ, Blanco Mendez J. Transdermal delivery of methotrexate: iontophoretic delivery from hydrogels and passive delivery from microemulsions. Int J Pharm 2001;215:57–65.

Das MK, Ahmed AB. Skin permeation enhancement effects of ascorbic acid and triethyl citrate on rofecoxib. Malay J Pharm Sci 2008;6:69-86.

Krishnaiah YSR, Satyanarayan V, Karthikcyan RS. Penetration enhancing an effect of menthol on the percutaneous flux of nicardipin hydrochloride through excised rat epidermis from hydroxypropyl cellulose gels. Pharm Dev Technol 2002;7:305–15.

Babita K, Kumar V, Rana V, Jain S, Tiwary AK. Thermotropic and spectropic behavior of skin: Relationship with percutaneous permeation enhancement. Curr Drug Delivery 2006;3:95–113.

Goats CY, Knutson K. Enhanced permeation of polar compounds through human epidermis. I. Permeability and membrane structural changes in the presence of short chain alcohols. Biochem Biophys Acta 1994;1195:169–79.

Yamune MA, Williams AC, Barry BW. Terpenes penetration enhancers in propylene glycol/water co-solvent systems: effectiveness and mechanism of action. J Pharm Pharmacol 1995;47:978–89.

Cornwell P, Barry BW. Wide angle x-ray diffraction of human stratum corneum effect of hydration and terpene enhancer treatment. J Pharm Pharmacol 1994;46:938–50.

Krishnaiah YSR, Bhaskar P, Satyanarayana V. Penetration-enhancing effect of ethanol-water solvent system and an ethanolic solution of carvone on transdermal permeability of nimodipine from HPMC gel across rat abdominal skin. Pharm Dev Technol 2004;9:63–74.

Published

07-03-2019

How to Cite

Ahmed, A. B., & Das, G. (2019). EFFECT OF MENTHOL ON THE TRANSDERMAL PERMEATION OF ACECLOFENAC FROM MICROEMULSION FORMULATION. International Journal of Applied Pharmaceutics, 11(2), 117–122. https://doi.org/10.22159/ijap.2019v11i2.30988

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Original Article(s)