EFFECT OF PENETRATION ENHANCER ON THE IN VITRO EX VIVO PERMEATION OF DICLOFENAC GEL
Abstract
Â
 Objective: The objective of this study was to compare and evaluate in vitro ex vivo transdermal potential of the diclofenac sodium (DS) gel by different permeation enhancers using Franz-type diffusion cells.
Methods: DS gel was prepared with carbapol, dimethyl sulfoxide, oleic acid (OA), and menthol with 1% w/w concentration each as the penetration enhancer. The in vitro, ex vivo permeability were determined using cellophane membrane and abdominal rat skin. Steady-state flux, permeability coefficient (kp), diffusion coefficient, and lag time were calculated.
Results: Menthol, at the concentration of 1% w/w, shows maximum kp, diffusion coefficient permeation enhancement effect with an enhancement ratio 40%, as compared to dimethyl sulfoxide and OA.
Conclusion: This finding predicts that DS gel 1% w/w containing menthol 1% w/w can possibly deliver therapeutically relevant dose of DS.
Keywords: Diclofenac sodium gel, Menthol, Penetration enhancer, Permeation coefficient.
Â
Â
Downloads
References
Ranade VV. Drug delivery systems transdermal drug delivery. J Clin Pharmacol 1991;31:401-18.
Bruton LL, Laza JS, Parker KL. Goodman Gilman’s; The Pharmacological Basis of Therapeutics. New York: McGraw Hill Medical Publishing Division; 2006. p. 801-10.
McCarthy DM. Comparative toxicity of nonsteroidal anti-inflammatory drugs. Am J Med 1999 13;107(6A):37S-46.
Mitchell JA, Warner TD. Cyclo-oxygenase-2: Pharmacology, physiology, biochemistry and relevance to NSAID therapy. Br J Pharmacol 1999;128(6):1121-32.
John VA. The pharmacokinetics and metabolism of diclofenac sodium (Voltarol) in animals and man. Rheumatol Rehabil 1979;Suppl 2:22-37.
Willis JV, Kendall MJ, Flinn RM, Thornhill DP, Welling PG. The pharmacokinetics of diclofenac sodium following intravenous and oral administration. Eur J Clin Pharmacol 1979;16(6):405-10.
Goosen C, du Plessis J, Mller DG, Janse van Rensburg LF. Correlation between physicochemical characteristics, pharmacokinetic properties and transdermal absorption of NSAIDs. Int J Pharm 1998;163:203-9.
Takahashi K, Suzuki T, Sakano H, Mizuno N. Effect of vehicles on diclofenac permeation across excised rat skin. Biol Pharm Bull 1995;18(4):571-5.
Escribano E, Calpena AC, Queralt J, Obach R, Doménech J. Assessment of diclofenac permeation with different formulations: Anti-inflammatory study of a selected formula. Eur J Pharm Sci 2003;19(4):203-10.
Aungst BJ. Fatty acids as skin permeation enhancers: In: Percutaneous Penetration Enhancers. 1st ed. Boca Raton: CRC Press; 1995. p. 247-70.
Sera VV, Raman VN. In vitro skin absorption and drug release. Indian Pharm 2006;73:356-60.
Francoeur ML, Golden GM, Potts RO. Oleic acid: Its effects on stratum corneum in relation to (trans) dermal drug delivery. Pharm Res1990;7(6):621-7.
Franz TJ, Lehman PA, Kagyand MK. Dimethylsulfoxide. In: Percutaneous Penetration Enhancers. Boca Raton: CRC Press; 1995. p. 148-67.
Hashida M, Yamashita F. Terpenes as penetration enhancers. In: Percutaneous Penetration Enhancers. Boca Raton: CRC Press; 1995. p. 280-95.
Baviskar DT, Biranwar YA, Bare KR, Parik VB, Sapate MK, Jain DK. In vitro and in vivo evalution of diclofenac sodium gel prepared with cellulose ether and carbopol 934P. Trop J Pharm Res 2013;12(4):489 94.
Babar A, Solanki UD, Cutie AJ, Plakogiannis F. Piroxicam release from different dermatological bases: In-vitro studies using cellophane membrane and hairless mouse skin. Drug Dev Ind Pharm 1990;16:523 40.
Higuchi WI. Analysis of data on the medicament release from ointments. J Pharm Sci 1962;51:802-4.
Shargel L, Wu-Pong S, Yu AB. Multiple-dosage regimens. In: Applied Biopharmaceutics & Pharmacokinetics. New York: McGraw-Hill; 2005. p. 254-80.
Walters KA. Penetration enhancers and their use in transdermal therapeutic system. In: Transdermal Drug Delivery Developmental Issues and Research. New York: Dekker; 1989. p. 78-87.
Naik A, Pechtold LA, Potts RO, Guy RH. Mechanism of oleic acid-induced skin penetration enhancement in vivo in humans. J Control Release 1995;37:299-306.
Shivhare DU, Jain BK, Mathur BV, Bhusari PK, Roy AA. Formulation development and evaluation of diclofenac sodium gel using water soluble polyacrylamide polymer. Dig J Nanomater Biostructure 2009;4:285-90.
Dey S, Mazumdar B, Patel JR. Enhance percutaneous permeability of acyclovir by DMSO from topical gel formulation. Int J Pharm Sci Drug Res 2009;1:13-8.
Takahashi K, Sakano H, Yoshida M, Numata N, Mizuno N. Characterization of the influence of polyol fatty acid esters on the permeation of diclofenac through rat skin. J Control Release 2001;73(2 3):351-8.
Nokhodchi A, Sharabiani K, Rashidi MR, Ghafourian T. The effect of terpene concentrations on the skin penetration of diclofenac sodium. Int J Pharm 2007 20;335(1-2):97-105.
Brain KR, Green DM, Dykes PJ, Marks R, Bola TS. The role of menthol in skin penetration from topical formulations of ibuprofen 5% in vivo. Skin Pharmacol Physiol 2006;19(1):17-21.
Arellano A, Santoyo S, Martin C, Ygartua P. Enhancing effect of terpenes on the in vitro percutaneous absorption of diclofenac sodium. Int J Pharm 1996;130:141-5.
Kunta JR, Goskonda VR, Brotherton HO, Khan MA, Reddy IK. Effect of menthol and related terpenes on the percutaneous absorption of propranolol across excised hairless mouse skin. J Pharm Sci 1997;86(12):1369-73.
Cordero JA, Camacho M, Obach R, Domenech J, Vila L. In vitro based index of topical anti-inflammatory activity to compare a series of NSAIDs. Eur J Pharm Biopharm 2001;51(2):135-42.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.