Effect of various penetration enhancers concentrations on diclafenac sodium release from cellulose acetate phthalate polymeric film

El-Nahas Hanan, Ghazy Fakhry, El-Ghamry Hanaa, Sabry Shereen

Abstract


An investigation was conducted to evaluate the influence of different penetration enhancers in various concentrations on the release of diclofenac sodium (DFS) as a water-soluble drug from Cellulose acetate phthalate polymeric films
containing 50% w/w PEG 600 as plasticizer, to choose the most appropriate enhancer and its optimum concentration to be used to achieve the maximum release and permeation of the drug. The addition of various enhancers, as isopropylmyristate (IPM; 0.2_5% w/w), oleic acid (OA; 0.2_5% w/w) and linoleic acid (LOA; 0.2_5% w/w), Tween 80 (T80;1_10% w/w) and transcutol, (TC; 1_10% w/w) enhanced the DFS release from the polymeric films. The enhancement ratio of the penetration enhancers used in the formulation of DFS were found to increase in the order of IPM>LOA>OA>T80>TC.
(56.2, 54.1, 50, 48.7 and 48%, respectively). In vitro permeation studies were performed using rabbit abdominal skin as the permeating membrane. The results indicated that maximum permeation was obtained at 24hrs (0.5% IPM, 0.2% LOA, 1% OA, 0.5% T80 and 10% TC, increased skin permeation of DFS by 4.46, 4.06, 3.37, 1.65 and 1.49 time, respectively). IPM was found to be the most efficient enhancer. The results obtained from ANOVA test indicate that the difference in drug permeation rates is highly significant compared to the control formulation (P<0.05). The mechanism of drug release from
the polymeric films obey Higuchi’s model.


Full Text:

PDF

References


Benson HA. Transdermal drug delivery: Penetration enhancement

techniques. Curr Drug Deliv 2005;2:23-33.

Kumar R, Philip A. Modified transdermal technologies: Breaking the

barriers of drug permeation via the skin. Trop J Pharma Res 2007;6:633-44.

Denyer SP, Guy RH, Hadgraft J, Hugo WB. The microbial degradation

of topically applied drugs. Int J Pharm 1985;26:89-97.

Pannatier A, Jenner P, Testa B, Etter JC. The skin as a drug metabolizing

organ. Drug Metab Rev 1978;8:319-43.

Choi HG, Rhee JD, Yu BK, Yong CS. The Effect of Enhancers on the

Penetration of Clenbuterol through Hairless Mouse Skin. J Korean

Pharm Sci 2003;33:29-36.

Mukherjee B, Mahapatra SK, Das S, Patra B. Sorbitan Monolaurate 20

as a Potential Skin Permeation. J Appl Res 2005;1:96-108.

Xiangqun Xu, Qiuhong Zhu. Evaluation of skin optical clearing

enhancement with Azone as a penetration enhancer. Opt Commun

;279223-8.

Panigrahi L, Pattnaik, S, Ghosal SK. The effect of pH and organic ester

penetration enhancers on skin permeation kinetics of terbutaline

sulfate from pseudolatex-type transdermal delivery systems through

mouse and human cadaver skins. AAPS Pharm Sci Tech 2005;6:167-73.

Shaila L, Pandey S, Udupa N. Design and evaluation of matrix type and

membrane controlled transdermal delivery systems of nicotine suitable

for use in smoking cessation. Indian J Pharm Sci 2006: 68: 179-84

Bijaya G, Harivardhan RL, Raghvendra VK, Jasmina K. Comparison of

skin permeability of drugs in mice and human cadaver skin. Indian J

Exp Biol 2000;l38:42-5.

Hanan MM. PhD. Thesis, Faculty of Pharmacy. Egypt: Zagazig University; 2001.

Wade Hull MS. Heat-enhanced transdermal drug delivery: A survey

paper. J Appl Res 2002;2:1-9.

Krishnaiah YS, Chandrasekhar DV, Rama B, Jayaram B, Satyanarayana

V, Al-Saidan SM. In vitro evaluation of limonene-based transdermal

therapeutic system of nicorandil in healthy human volunteers. Skin

Pharmacol Physiol 2004;18:263-72.

Dhanikula AB, Panchagnula R. Development and characterization of

biodegradable chitosan films for local delivery of Paclitaxel. AAPS J

;6:e27.

Heng PW, Chan LW, Ong KT. Influence of storage conditions and type

of plasticizers on ethylcellulose and acrylate films formed from aqueous

dispersions. J Pharm Sci 2003;6:334-44.

Venkateshwari Y, Jayachandra RB, Sampath Kumar D, Mittal N, Pandit

JK. Development of low coast tetracycline strip for long term treatment

of periodontal disease. Indian Drugs 1995;32:205-9

Mohamed A, Yasmin S, Asgar A. Matrix type transdermal drug delivery

systems of metoprolol tartrate: In vitro characterization. Acta Pharm

;53:119-25.

Shah HS, Tojo K, Chien YW. T0 ransdermal controlled delivery of

verapamil: Characterization of in vitro skin permeation. Int J Pharm

;86:167-73.

Squillante E, Needham T, Zia H. Solubility and in vitro transdermal

permeation of nifedipine. Int J Pharm 1997;159:171-80.

Ghosh TK, Adir J, Xiang S, Onyilofur S. Transdermal delivery of

Metoprolol II: In vitro skin permeation and bioavailability in hairless

rats. J Pharm Sci 1995;84:158-60

Libermann, Lachman. Pharmaceutical dosage forms. 2 nd ed.

Philadelphia, PA: Lea and Febiger; 1990. p. 265.

Winter GA, Risley EA, Nuss GW. Carrageenin-induced edema in hind

paw of the rat as an assay for antiiflammatory drugs. Proc Soc Exp Biol

Med 1962;111:544-7.

Sang CC, Wonjun H. Anti-inflammatory activity of ketoprofen gel on

carrageenan-induced paw edema in rats. J Pharm Sci 1990;79:974-7.

Wu T, Pan W, Chen J, Zhang R. Studies of the drug permeability and

mechanical properties of free films prepared by cellulose acetate

pseudolatex coating system. Drug Dev Ind Pharm 2001;26:95-102.

Heng PW, Chan LW, Ong KT. Influence of storage conditions and type of

plasticizers on ethylcellulose and acrylate films formed from aqueous

dispersions. J Pharm Pharm Sci 2003;6:334-44.

Verma PR, Murthy TE. Transdermal flurbiprofen delivery using HPMC

matrices: Design, in vitro and in vitro evaluation. Drug Dev Ind Pharm

;23:633-8.

Leichtnam ML, Rolland H, Wüthrich P, Guy RH. Identification of

penetration enhancers for testosterone transdermal delivery from

spray formulations. J Control Release 2006;113:57-62.

Saunders J, Davis H, Coetzee L, Botha S, Kruger A, Grobler A. A novel

skin penetration enhancer: Evaluation by membrane diffusion and

confocal microscopy. J Pharm Pharmaceut Sci 1999;2:99-107.

Sarisuta N, Saowakontha R, Ruangsuksriwong, C. Effects of surfactant

on release characteristics of clonidine hydrochloride from ethylcellulose

film. Drug Dev Ind Pharm 1999;25:373-7.

Mortazavi SA, Aboofazeli R. Investigation into the effect of various

penetration enhancers on percutaneous absorption of piroxicam.

Iranian J Pharma Res 2003;2:135-40.

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

a clonazepam Transdermal permeation enhancer hydrophilic gel

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

Karandea P, Mitragotrib S. Enhancement of transdermal drug

delivery via synergistic action of chemicals. Biochim Biophys Acta

;1788:2362-73.




DOI: http://dx.doi.org/10.22377/ajp.v5i1.82

Refbacks

  • There are currently no refbacks.