in- vitro release, thermodynamics and pharmacodynamic studies of aceclofenac transdermal eudragit patches
Date
2009
Journal Title
Journal ISSN
Volume Title
Type
Article
Publisher
Drug Invention Today
Series Info
drug invention today;Volume: 1 Issue: 1
Doi
Scientific Journal Rankings
Abstract
Aceclofenac, a nonsteroidal anti-inflammatory drug has been formulated into transdermal Eudragit patches. The drug was first characterized
for its physicochemical properties by studying its solubility and its partition coefficient at different pH values. Formulation of Aceclofenac
into transdermal patches using three acrylic resin polymers like Eudragit L100, L100-55 and S100 was done. The effect of different plasticizers,
like propylene glycol (PG) and polyethylene glycol (PEG 400) in concentrations of 5% and 10%, on the in-vitro drug release was investigated.
Thermodynamics of the in-vitro release of Aceclofenac from Eudragit patches were also studied. The anti-inflammatory effect of the selected
Aceclofenac Eudragit patches was determined in male albino rats, using paw edema method. The results of the in-vitro release show that,
Eudragit patches of Aceclofenac had an acceptable % drug release after 60 minutes and the increase of hydrophilic plasticizers PG or PEG
concentrations form 5% to 10% is accompanied by an increase in drug release. The release of drug from all investigated Eudragit patches
follows zero order kinetic and it increases linearly as a function of temperature. The free energy (rG) values of drug release are negative for
all Eudragit patches and the best thermodynamically stable patch was L100+10% PG, which was chosen for further pharmacodynamic
evaluation of Aceclofenac anti-inflammatory activity. The results show that in all treated rat groups there are significant inhibition in edema
thickness, produced by carrageenan when compared with the non-treated group. This inhibition in edema is statistically significant at P <
0.05. It was also observed, that the group pretreated with water for 30 hours prior to the experiment showed the highest percent edema
inhibition, followed by group pretreated with isopropyl myristate (IPM). This study demonstrates the feasibility of formulating Aceclofenac
into transdermal patches using Eudragit L100+10% PG to deliver it as part of inflammatory management.
Description
MSA Google Scholar
Keywords
University of Transdermal Eudragit patches, Aceclofenac, Plasticizers, In-vitro release, Thermodynamics, Anti-inflammatory activity
Citation
1. Yomazaki R, Kawai S, Matsuzaki, T, Kaneda, N, Hashimoto S, Yokokura T, Okamoto R, Koshino T, Mizushima Y. Aceclofenac blocks prostaglandin E2 production following its interacellular conversion into cyclooxygenase inhibitors. Eur. J. Pharmacol. 329, 1997, 181-187. 2. Barry BW, in “Dermatological Formulation: Percutaneous Absorption”, Barry BW. (ed.), Marcel Dekker, Inc., NewYork. 1996, p. 521. 3. Nasr M, Mansour S, Mortada ND, El-Shamy AA. Lipospheres as carriers for Topical Delivery of Aceclofenac Preparation, Characterization and In-Vivo Evaluation. AAPS Pharm.Sci.Tech. 9, 2008, 154- 162. 4. Shakeel F, Baboota S, Ahuja A, Ali J, Aqil J, Shafik S. Nanoemulsions as Vehicles for Transdermal Delivery of Aceclofenac. AAPS Pharm.Sci.Tech. 8, 2007, E1-E9. 5. Yang JH, Kim Y, Kim K M. Preparation and evaluation of aceclofenac microemulsion for transdermal delivery system. Arch. Phrm. Res. 25, 2002, 534-540. 6. El-Gendy NA, Sabry NA, El-Attar M, Omar E, Mahmoud M. Transdermal patch incorporating salbutamol sulphate: In-vitro and Drug Invention Today Vol.1.Issue 1.November 2009 Maha Abd El-Hamid Marzouk et al. / Drug Invention Today 2009, 1(1),16-22 16-22 clinical characterization. Drug Discov. Ther. 2, 2008, 219-228. 7. Shah HS, Tojo K, Chien Y W. Transdermal controlled delivery of verapamil: characterization of in-vitro skin permeation, In. J. Pharm. 86, 1992, 167-173. 8. Pozzo AD, Donzelli G, Liggeri E, Rodriguez L. Percutaneous absorption of nicotinic acid derivatives in-vitro. J. Pharm. Sci., 80, 1991, 54-57. 9. Arora P, Mukherjee B. Design, development, physicochemical, and in-vitro and in-vivo evaluation of transdermal patches containing diclofenac diethylammonium salt. J. Pharm. Sci, 91, 2002, 2076- 2089. 10. Aqil M, Sultana Y, Ali A, Hamdard H. Matrix Type Transdermal Drug Delivery Systems of Metoprolol Tartrate: In-Vitro Characterization. Acta. Pharm. 53, 2003, 119-125. 11. Eouani C, Piccerelle PH, Pinderre P, Bourret E, Joachim J. In-vitro comparative study of buccal mucoadhesive performance of different polymeric films. Eur. J. Pharm. Biopharm. 52, 2001, 45-55. 12. Kibbe AH. in “Hand Book of Pharmaceutical Excipients”, 3rd ed., American Pharmaceutical Association, Washington, DC., 2000, pp. 401-406. 13. Liebowitz SM, Ichizuka K, McGinity J W. Physicochemical factors influencing drug release from acrylic resin films. in “Pharmaceutical Technology: Controlled Drug Release”, Vol.1 Rubinstin, M H., Ellis Horwood Limited,1987, pp. 9-16. 14. Okor RS. Influence of hydrophilic character of plasticizers and polymer on certain film properties. Int. J. Pharm., 11, 1982, 1-9. 15. Azarmi S, Roa W, Löbenberg R. Current perspectives in dissolution testing of conventional and novel dosage forms. Int. J. Pharm. 328, 2007, 12-21. 16. Samuelov Y, Donbrow M, Friedman M. Sustained Release of Drugs From Ethylcellulose- Polyethylene Glycol Films and Kinetics of Drug Release. J. Pharm. Sci. 68, 1979, 325-329. 17. He Y, Wang Y, Tang L, Liu H, Chen W, Zheng Z, Zou G. Binding of Puerarin to Human Serum Albumin: A sectroscopic Analysis and Molecular Docking. J. Fluoresc. 18, 2008, 433-442. 18. Connors KA. in “Thermodynamics of Pharmaceutical Systems”, University of Wisconsin – Madison, John Wiley & Sons, Inc., Publication, Canada, 2002, pp. 116-125. 19. Behl RC, Barrett M. Hydration and percutaneous absorption II: Influence of hydration on water and alkanol permeation through swiss mouse skin, Comparison with hairless mouse. J. Pharm. Sci., 70, 1981, 1212-1215. 20. Shah VP, Behl CR, Flynn GL. Principle and criteria in the development and optimization of topical therapeutic products. Pharm. Res., 9, 1992, 1107-1111 21. Hadgraft J, Ridout G. Development of model membranes for percutaneous absorption measurements. I. Isopropyl myristate. Int. J. Pharm., 39, 1987, 149-156. 22. Sinko, PJ. “Martin’s Physical Pharmacy and Pharmaceutical Sciences,” 5th ed., Lippincott Williams & Wilkins, Baltimore, 2006, p. 210. 23. Shah VP, Tymes NW, Yamamoto LA, Skelly JP. In-vitro dissolution profile of transdermal nitroglycerin patches using paddle method. Int. J. Pharm. 32, 1986, 243-250. 24. Lim LY, Wan LSC. The effect of plasticizers on the properties of polyvinyl alcohol patches. Drug Dev. Ind. Pharm. 20, 1994, 1007- 1020. 25. Arellano A, Santoyo S, Martin C, Ygartua P. Influence of propylene glycol and isopropyl myristate on the in-vitro percutaneous penetration of diclofenac sodium from carbopol gels. Eur. J. Pharm. 7, 1998, 129–135.