FORMULATION AND EVALUATION OF ETODOLAC LECITHIN ORGANOGEL TRANSDERMAL DELIVERY SYSTEMS

Authors

  • Sahar M. Fayez Department of Pharmaceutics, Faculty of pharmacy, October 6 University,Giza, 6th October City, Egypt
  • Shadeed Gad Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt
  • El-sayed A. Khafagy Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt
  • Gehad A. Abdel Jaleel Department of Pharmacology, National Research Centre,El-Bohoth St.,Dokki,Cairo, Egypt
  • Mamdouh M. Ghorab Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt
  • Sohier A. El-nahhas Department of Pharmaceutics, Faculty of pharmacy, October 6University, 6th October City, Giza, Egypt

Keywords:

Etodolac, Lecithin, Organogels, Permeation, In vivo study

Abstract

Objective: Etodolac (ETD) is a non-steroidal anti-inflammatory drug used for the acute and chronic treatment of rheumatoid arthritis. It exhibits poor water solubility so its bioavailability is limited. Long term use of ETD causes serious gastrointestinal disturbance. Lecithin organogels (Los) have generated considerable interest over the years as potential topical drug delivery vehicle. Therefore, the objective of this study was to formulate ETD in lecithin organogels as a transdermal delivery system.

Methods: Based on the preliminary studies, pseudoternary phase diagrams were constructed using isopropyl myristate (IPM), water and lecithin as a surfactant with different cosurfactants (CoS) and organogel areas were identified and three systems each of 36 formulae were prepared. A number of organogels were selected and loaded with 1% ETD then evaluated for visual inspection, spreadability, pH, rheological and in vitro release studies to select the optimum formulae. The selected formulae were subjected to ex-vivo permeation through excised abdominal rabbit skin and their stability was studied for one year of storage under ambient conditions. The therapeutic efficacy of ETD including analgesic activity and anti-inflammatory effect was monitored.

Results: The prepared ETD organogels showed suitable properties for topical application and the selected formulae (F3, F14 & F39) showed enhanced permeation. The In vivo study showed a significant difference in the therapeutic efficacy of formula F14, containing 10% IPM, 40% lecithin/PG in the ratio of (5:1) and 50% water, compared to a market product. Skin irritation test and histopathological studies proved the safety of this formula.

Conclusion: So this organogel formula (F14) is considered to be a potential vehicle for a sustained release transdermal delivery system for ETD.

 

Downloads

Download data is not yet available.

References

Sinha VR, Chadha AR, Goel H. Enhancing the dissolution of hydrophobic guests using solid state inclusion complexation: characterization and in vitro evaluation. J Inclusion Phenom 2010;66(3):381-92.

Reynolds J. Martindale, the extra pharmacopeia. 31st ed. London: Royal Pharmaceutical Society; 1996.

Barakat NS. Etodolac-Liquid-Filled dispersion into hard gelatin capsules : an approach to improve dissolution and stability of etodolac formulation. Drug Des Discov 2009;32:865–76.

Changez M, Varshney M, Chander J, Dinda AK. Effect of the composition of lecithin/n-propanol/isopropyl myristate/water microemulsions on barrier properties of mice skin for transdermal permeation of tetracaine hydrochloride: in vitro. Colloids Surf B 2006;50(1):18–25.

Sharma N, Agarwal G, Rana AC, Bhat ZALI, Kumar D. Transdermal drug delivery system: a tool for novel drug delivery system. Int J Drug Dev Res 2011;3(3):70–84.

Saroha K, Yadav B, Sharma B. Transdermal patch: A discrete dosage form. Int J Curr Pharm Res 2011;3:98–103.

Cevc G, Paltauf E. Phospholipid Characterization, Metabolism and Novel Biological Applications. Champaign, AOCS Press; 1995.

Zarif L. Elongated supramolecular assemblies in drug delivery. J Control Release 2002;81:7–23.

Kumar R, Katare OP. Lecithin organogels as a potential phospholipid-structured system for topical drug delivery: a review. Aaps Pharm Sci Tech 2005;6(2):E298–310.

Schurtenberger P, Scartazzini R, Magid LJ, Leser ME, Luisi PL. structural and dynamic properties of polymer-like reverse micells. J Phys Chem 1990;94:3695–701.

El-Laithy H. Self-nanoemulsifying drug delivery system for enhanced bioavailability and improved hepatoprotective activity of biphenyl dimethyl dicarboxylate. Curr Drug Deliv 2008;5:170–6.

Badawi AA, Sakran WS, Ramadan MA. Improvement of the microbiological activity of topical ketoconazole using microemulsion systems. J Drug Del Sci Tech 2012;22(6):473–8.

Pathan IB, Setty CM. Enhancement of transdermal delivery of tamoxifen citrate using nanoemulsion vehicle. Pharm Tech 2011;3(1):287–97.

Pandey M, Belgamwar V, Gattani S, Surana S, Tekade A. Pluronic lecithin organogel as a topical drug delivery system. Drug Deliv 2010;17(1):38–47.

Nour SA, Shalaby SH, Afify NN, Abd El-Aal S, MMK. Formulation and evaluation of econanazole nitrate emulgels. J Drug Res Egypt 2002;24(1-2):63–71.

Soliman SM, Abdel Malak NS, El-Gazayerly ON, Abdel Rehim aa. Formulation of microemulsion gel systems for transdermal delivery of celecoxib: In vitro permeation, anti-inflammatory activity and skin irritation tests. Drug Discoveries Ther 2010;4(6):459–71.

Draize J, Woodward G, Calvery H. Methods for the study of irritation and toxicity of substances applied topically to the skin and mucous membranes. J Pharmacol Exp 1944;82:377–9.

Koster R, Anderson M, De-Beer EJ. Acetic acid analgesic screen. Fed Proc 1959;18:418–20.

Adzu B, Amos S, Wambebe C, Gamaniel K. Anti-nociceptive activity of the aqueous extract of Zixyphus spina-christi root bark. Fitoterapia 2001;72:344–50.

Young JM, Luo Y, Cheng H, Hsieh W, Liao J, Peng W. Analgesic and anti-inflammatory activities of (6)-gingerol. J Ethnopharmacol 2005;96:207–10.

Winter CA, Risley EA, Nuss GW. Carrageenin induced oedema in hind paws of the rats as an assay for anti-inflammatory drugs. Proc Soc Exp Biol Med 1962;111:544–7.

Abbas NA. A Biopharmaceutical study on the anti-inf lammatory drug Nimesulide. Master thesis, department of Pharmaceutics, Suez Canal University; 2011. p. 48–9.

Banchroft JD, Stevens A, Turner DR. Theory and practice of histological techniques. Fourth Ed. Churchil Livingstone, New York, London, San Francisco, Tokyo; 1996.

Thorat SP, Rane SI. Formulation and in vitro evaluation of lecithin (soya and egg) based aceclofenac organogels. J Pharm Res 2010;3(6):1438–41.

Sinko PJ. Rheology martin’s physical pharmacy and pharmaceutical sciences. 5th ed. Lippincott Williams & Wilkins; 2006.

Ozguney IS, Karasulu HY, Kantarci G, Sozer S, Guneri T, Ertan G. Transdermal delivery of declofenac sodium through rat skin from various formulations. AAPS Pharm Sci Tech 2006;7:E39–45.

Huang YC, Tsai SK, Wang MH, Lin PL, Chen LK, Lin CJ, et al. Intravenous tenoxicam reduces uterine cramps after cesarean delivery. Can J Anaesth 2002;49:384–7.

Collier HOJ, Dinneen LC, Johnson CA, Schneider C. The abdominal constriction response and its suppression by analgesic drugs in the mouse. Br J Pharmacol 1968;32:295–310.

Agrawal V, Gupta V, Ramteke S, Trivedi P. Preparation and evaluation of tubular micelles of pluronic lecithin organogel for transdermal delivery of sumatriptan. AAPS Pharm Sci Tech 2010;11(4):1718–25.

Van Buskirk GA, Gonzalez MA, Shah VP, Barnhardt S, Barrrett C, et al. Scale-up of adhesive transdermal drug delivery systems. Pharm Res 1997;14(7):848–52.

Published

01-04-2015

How to Cite

Fayez, S. M., S. Gad, E.- sayed A. Khafagy, G. A. A. Jaleel, M. M. Ghorab, and S. A. El-nahhas. “FORMULATION AND EVALUATION OF ETODOLAC LECITHIN ORGANOGEL TRANSDERMAL DELIVERY SYSTEMS”. International Journal of Pharmacy and Pharmaceutical Sciences, vol. 7, no. 4, Apr. 2015, pp. 325-34, https://mail.innovareacademics.in/journals/index.php/ijpps/article/view/5154.

Issue

Section

Original Article(s)

Most read articles by the same author(s)