Optimization of physical characterization, skin permeation of naproxen from glycofurol-based topical gel

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Nahla S Barakat


In view of good skin tolerability, glycofurol was used as a vehicle-based gel and its effect on the topical penetration of Naproxen (NAP) was investigated. The aim of this study was to develop a suitable gel with bioadhesive property,
spreadability, and viscosity for a topical anti-inflammatory effect.Three gelling agents were examined: Carbopol 974P, Gantrez  AN 119, and Polyvinylpyrroloidone PVP K30. Skin permeation rates and lag times of NAP were evaluated using the Franz- type diffusion cell, in order to optimize gel formulation. The permeation rate of the NAP-based gel across excised rat skin
was investigated. A significant increase in permeability parameters such as steady-state flux (Jss), permeability coefficient (Kp), and penetration index (PI) were observed in the optimized formulation containing 2% Transcutol as a permeation enhancer. From the skin irritation test, it was concluded that the optimized novel tetraglycol-based gel formulation was safe to be used for transdermal drug delivery. The developed naproxen / glycofurol-based gel appeared promising for dermal and transdermal delivery of naproxen and could be applicable with water-insoluble drugs, which would circumvent most
of the problems associated with drug therapy.


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Barakat, N. S. (2014). Optimization of physical characterization, skin permeation of naproxen from glycofurol-based topical gel. Asian Journal of Pharmaceutics (AJP), 4(2). https://doi.org/10.22377/ajp.v4i2.140


Mitchell JA, Warner TD. Cyclooxygenase-2: Pharmacology, physiology,

biochemistry and relevance to NSAID therapy. Br J Pharmacol


Vaile JH, Davis P. Topical NSAIDs for musculoskeletal conditions: A

review of the literature. Drugs 1998;56:783-99.

Burnham R, Gregg R, Healy P. The effectiveness of topical diclofenac

for lateral epicondylitis. Clin J Sports Med 1998;8:78-81.

Moore RA, Tramer MR, Carroll D. Quantitive systematic review of

topically applied non-steroidal anti-inflammatory drugs. Br Med J


Monteiro-Riviere NA, Inman AD, Riviere JE, McNeill SC, Francoeur ML.

Topical penetration of piroxicam is dependent on the distribution of

the local cutaneous vasculature. Pharm Res 1993;10:1326-31.

Huang YB, Wu PC, Ko HM, Tsai YH. Cardamon oil as a skin permeation

enhancer for indomethacin, piroxicam and diclofenac. Int J Pharm


Yokomozo Y, Sagitani H. Effects of phospholipids on the percutaneous

penetration of indomethacin through the dorsal skin of guinea pig in

vitro. J Control Release 1996;38:267-74.

Singh P, Roberts MS. Skin permeability and local tissue concentration

of nonsteroidal anti-inflammatory drugs after topical application. J

Pharmacol Exp Ther 1994;268:44-151.

Sioufi A, Pammer F, Boschet F. Percutaneous absorption of diclofenac

in healthy volunteers after single and repeated topical application of

diclofenac emugel. Biopharm Drug Dispos 1994;15:441-9.

Giuliano F, Warner TD. Ex vivo assay to determine the cyclooxygenase

selectivity of non-steroidal anti-inflammatory drugs. Br J Pharmacol


Bonina FP, Puglia C, Barbuzzi T, De Caprariis P, Palagiano F, Rimoli

MG, et al. In vitro and in vivo evaluation of polyoxyethylene esters as

dermal prodrugs of ketoprofen, naproxen and diclofenac. Eur J Pharm

Sci 2001;14:123-34.

Glavas-Dodov M, Goracinova K, Mladenovska K, Fredro-Kumbaradzi E.

Release profile of lidocaine HCl from topical liposomal gel formulation.

Int J Pharm 2002;242:381-4.

Pabla D, Zia H. A comparative permeation/release study of different

testosterone gel formulations. Drug Deliv 2007;14:389-96.

Sharma NC, Galustians HJ, Qaquish J, Galustians A, Rustogi KN, Petrone ME, et al. The clinical effectiveness of a dentifrice containing triclosan and a copolymer for controlling breath odor measured organolepticallytwelve hours after tooth brushing. J Clin Dent 1999;10:131-4.

Arbos P, Wirth M, Arangoa MA, Gabor F, Irache JM. Gantrez AN as a

new polymer for the preparation of ligand-nanoparticle conjugates. J

Control Release 2002;83:321-30.

Shin SC, Cho CW, Choi HK. Permeation of piroxicam from the poloxamer gels. Drug Dev Ind Pharm 1999;25:273-8.

Bonacucina G, Martelli S, Palmieri GF. Rheological, mucoadhesive and

release properties of carbopol gels in hydrophilic cosolvents. Int J

Pharm 2004;282:115-30.

Shin SC, Lee JW, Yang KH, Chi H, Lee CH. Preparation and evaluation

of bioadhesive benzocaine gels for enhanced local anesthetic effects.

Int J Pharm 2003;260:77-81.

Lardy F, Vennat B, Pouget P, Pourrat A. Functionalization of

hydrocolloids: Principal component analysis applied to the study

of correlations between parameters describing the consistency of

hydrogels. Drug Dev Ind Pharm 2000;26:715-21.

Contreras MD, Sanchez M. Application of a factorial design to the study

of the flow behavior, spreadability, transparency of Carbopol ETD 2020

gel. Part II. Int J Pharm 2002;234:149-57.

Kleck CM. Gels and jellies. In: Swarbrick J, Boyland JC, editors.

Encyclopedia of Pharmaceutical Technology. Vol. 6. New York: Mercel

Dekker; 1992. p. 415-39.

Provost C, Herbost H, Kinget R. Transparent oil-water gels: Study of

some physico-chemical and biopharmaceutical characteristics. Part 3:

Viscosity and conductivity measurements. Pharm Ind. 1988;50:1190-5.

Martin AN, Banker GS, Chun AH. Rheology. In: Bean HS, Beckett AH,

Carless JE, editors. Advances in Pharmaceutical Sciences. Vol. 1. New

York: Academic Press; 1967. p. 1-85.

Prentice JH. Measurements in the rheology of foodstuffs. London:

Elsevier; 1984.

Balzer D, Varwig S, Weihrauch M. Viscoelasticity of personal care

products. Coll Surf A Phys Eng Aspects 1995;99:233-46.

Fang JY, Fang CL, Hong CT, Chen HY, Lin TY, Wei HM. Capsaicin and

nonivamide as novel skin permeation enhancers for indomethacin. Eur

J Pharm Sci 2001;12:195-203.

Suwanpidokkul N, Thongnopnua P, Umprayn K. Transdermal delivery

of zidovudine (azt): The effects of vehicles, enhancers, and polymer

membranes on permeation across cadaver pig skin. AAPS PharmSciTech


Meidan VM, Al_Khallil M, Michniak BB. Enhanced iontophoretic

delivery of buspirone hydrochloride across human skin using chemical

enhancers. Int J Pharm 2003;264:73-83.

Patel SR, Zhong H, Sharma A, Kalia YN. In vitro and in vivo evaluation

of the transdermal iontophoretic delivery of sumatriptan succinate.

Eur J Pharm Biopharm 2007;66:296-301.

Tas C, Ozkan Y, Savaser A, Baykara T. In vitro release studies of

chlorpheniramine maleate from gels prepared by different cellulose

derivatives. Farmaco 2003;58:605-11.

Namdeo A, Jain NK. Liquid crystalline pharmacogel based enhanced

transdermal delivery of propranolo hydrochloride. J Control Release


Mutalik S, Udupa N. Glibenclamide transdermal patches:

Physicochemical, pharmacodynamic, and pharmacokinetic evaluations.

J Pharm Sci 2004;3:1577-94.

Ugweke MI, Verbeke N, Kinget R. The biopharmaceutical aspects of

nasal mucoadhesive drug delivery. J Pharm Pharmacol 2001;53:3-22.

Ho HO, Huang FC, Sokoloski TD, Sheu MT. The influence of cosolvents

on the in vitro percutaneous penetration of diclofenac sodium from gel

system. J Pharm Pharmacol 1994;46:636-42.

Barry BW. Properties that influence percutaneous absorption, Chapter

In: Barry BW (Edt), Dermatological Formulations. Percutaneous

Absorption. Vol. 18, New York: Dekker; 1983. p. 127-233.

Takahashi A, Suzuki S, Kawasaki N, Kubo W, Miyazaki S, Loebenberg

R, et al. Percutaneous absorption of non-steroidal anti-inflammatory

drugs from in situ gelling xyloglucan formulations in rats. Int J Pharm


Chow DS, Kaka I, Wang TI. Concentration dependent enhancement

of 1-dodecylazacycloheptan-2-one on the percutaneous penetration

kinetics of triamcinolone acetonide. J Pharm Sci 1984;73:1794-9.

Williams AC, Barry BW. Skin absorption enhancers. Crit Rev Ther Drug

Carrier Syst 1992;9:305-53.

Forslind B, Engstrom S, Enghlom J, Norlen L. A novel approach to

the understanding of human skin function. J Dermatol Sci 1997;14:


Mura P, Faucci MT, Bramanti G, Corti P. Evaluation of transcutol as a

clonazepam transdermal permeation enhancer from hydrophilic gel

formulations. Eur J Pharm Sci 2000;9:365-72.

Draize JH, Woodward G, Calvery HO. Methods for the study of irritation

and toxicity of substances applied topically to the shin and mucous

membranes. J Pharmacol Exp Ther 1944;82:377-9.