Abstract
To develop novel transdermal formulation for aceclofenac, microemulsion was prepared for increasing its skin permeability. Based on solubiity and phase studies, oil and surfactant was selected and composition was determined. Microemulsion was spontaneously prepared by mixing ingredients and the physicochemical properties such was investigated. The mean diameters of microemulsion were approximately 90 nm and the system was physically stable at room temperature at least for 3 months. In addition, the in vitro and in vivo performance of microemulsion formulation was evaluated. Aceclofenac was released from microemulsion in acidic aqueous medium, and dissolved amounts of aceclofenac was approximately 30% after 240 min. Skin permeation of aceclofenac from microemulsion formulation was higher than that of cream. Following transdermal application of aceclofenac preparation to delayed onset muscle soreness, serum creatine phosphokinase and lactate dehydrogenase activity was significantly reduced by aceclofenac. Aceclofenac in microemulsion was more potent than cream in the alleviation of muscle pain. Therefore, the microemulsion formulation of aceclofenac appear to be a reasonable transdermal delivery system of the drug with enhanced skin permeability and efficacy for the treatment of muscle damage.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Attwood D., Mallon C. and Taylor C.J., Phase studies on oil-in-water phospholipid microemulsions.Int. J. Pharm., 34, R5-R8 (1992).
Benoit P.W. and Belt W.D., Destruction and regeneration of skeletal muscle after treatment with a local anesthetics, bupivacaine.J. Anat., 107, 547–547 (1970).
Briggaman R.A., Biochemical composition of the epidermal-dermal junction and other basement membrane.J. Invest. Dermatol., 78, 1–6 (1982).
Charman S.A., Charman W.N. and Rogge M.C., Wilson T.D., Dutko F.J. and Pouton C.W., Self-emulsifying drug delivery system: Formulation and biopharmaceutic evaluation of an investigational lipophilic compound.Pharm. Res., 9, 87–93 (1992).
Constantinides P.P. and Yiv S.H., Particle size determination of phase inverted water-in-oil microemulsions under different dilution and storage conditions.Int. J. Pharm., 115, 225–234 (1995).
Cordero, J.A., Alarcon, L., Escribano, E., Obach, R. and Domenech, J., A comparative study of the transdermal penetration of a series of nonsteroidal antiinflammatory drugs.J. Pharm. Sci., 36(4), 503–508 (1997).
Cullander, C. and Guy, R. H., Routes of delivery: Case studies (6) delivery of peptides and proteins.Adv. drug delivery Rev., 8, 291–329 (1992).
Dixon M. and Webb E.,Enzymes, San Francisco, Academic press, 54–56 (1979).
Friberg S., Larsson M. and Mandell L., Mesomorphous phase, a factor of importance for the properties of emulsions.J. Coll. Int.Sci., 29(1), 155–155 (1969).
Friberg S., Microemulsions, hydrotropic solutions and emulsions, a question of phase equilibra.J. Am. Oil Chem. Society, 48, 149–149 (1970).
Friberg S. and Madell L., Phase equilibra and their influence on the properties of emulsions.J. Pharm. Sci., 59(7), 1001–1001 (1970).
Friberg S. and Madell L., Phase equilibra and their influence on the properties of emulsions.J. Am. oil Chem. Society, 48, 578–578 (1971).
Gasco P.F. and Lattanzi F.; Long-acting delivery systems for peptides: reduced plasma testosterone levels in male rats aftera single injection.Int. J. Pharm., 62, 119–123 (1990).
Grau M., Guasch J., Monter J.C., Felipe A., Carrasco E. and Tulia S., Pharmacology of the potent New non-steroidal antiinflammatory agent aceclofenac.Drug Res., 41(11). 1265–1276 (1991).
Gray J.E., Local histologic changes following long-term intramuscular injection.Arch. Pathol., 84, 522–522 (1967).
Greenberg I. and Arneson E., Experimental rhabdomyolysis with myoglobiuria in a large group of military trainees.Neurology, 17, 216–216 (1967).
Guy RH, Hadgraft J, Bucks DA., Transdermal drug delivery and cutaneous metabolism.
Hanzlikova V. and Gutmann E., Effect of ischemia on contractile and histochemical properties of rat soleus muscle.Pflugers Arch., 379, 209–209 (1979).
Janssen Degenarr C.P. and Geurten P., Plasma activity of muscle enzyme: Quantification of skeletal muscle damage & relationship with metabolic variables.Int. Spt. Med., 10, 15–17 (1988).
Javinen M., Healing of a crush injury in rat striated muscle: a histological study of the effect of early mobilization and immobilization on the repair process.Acta. Pathol. Microbiol. 2nd., 83, 269–269 (1975).
Jeppson R. and Ljunberg S., Anticonvulsant activity in mice of diazepam in an emulsion formulation for intravenous administration.Acta. Pharmacol. Toxicol., 36, 312–312 (1975).
Kale N.J. and Allen L.V., Studies on microemulsions using Brij 96 as surfactant and glycerin, ethylene glycol and propylene glycol as cosurfactants.Int. J. Pharm., 57, 87–93 (1989).
Knepp V.M., Hadgraft J. and Guy R.H., Transdermal drug delivery: problems and possibilities.Crit. Rev. Ther. Drug Carrier Syst., 4(1), 13–37 (1987).
Kronevi T. and Ljunberg S., Sequel following intra-arterially injected diazepam formulations.Acta Pharm. Suecica., 20, 389–389 (1983).
Lee G.W. and Jee U.K., Evaluation of various vehicle and o/w microemulsions of flurbiprofen as transdermal delivery system.J. Kor. Pharm. Sci., 28(3), 141–141 (1998).
Lee Y.E., The effect of different technique levels of man’s floor exercise on the change of activities of blood CPK, LDH and isozymes in gymnasts.Thesis of Physi. Educ. Kor. Nati. Univ., (1997).
Malcolmson C. and Lawrence A., Comparison of the incorporation of model steroids into non-ionic micellar and microemulsion systems.J. Pharm. Pharmacol., 45, 141–143 (1993).
Mcglynn G.H., Laughlin N.T. and Rowe V., Effect of loctromyographic feefback and static stretching on artificially induced muscle soreness.Am. J. Phys. Med., 58, 139–139 (1979).
Meltzer H.Y., Factors affecting serum CPK levels in the general population: the role of race, activity and sex.Clin. Chim. Acta., 33, 165–169 (1971).
Mizushima Y., Hamano T. and Yokoyama K., Use of a lipid emulsion as a novel carrier for corticosteroids.J. Pharm. Pharmacol., 34, 49–50 (1982).
Ohkuwa T. and Miharu M., Plasma LDH activity and LDH isoenzymes after 400m & 3,000m run in sprint & long distance runners.J. Sports Medi., 26, 362–368 (1986).
Raimondi G.A., Puy R.J. and Schwarz E.R., Rosenberg M., Effects of physical training on enzymatic activity of human skeletal muscle.Biomedicine, 22, 496–501 (1975).
Schulman J.H., and Friend J.A., Light scattering investigation of the structure of transparent oil-water disperse systems.J. Colloid Sci., 4, 497–497 (1949).
Sorvari T. and Jarvinen M., Healing of a crush injury in rat striated muscle: description and testing of a new method of inducing a standard injury to the calf muscles.Acta. Pathol. microbiol. 2nd., 83, 259–259 (1975).
Williams M.L. and Elias P.M., The extracellular matrix of stratum corneum: role of lipids in normal and pathological function.Crit Rev Ther Drug Carrier Syst., 3(2), 95–122 (1987).
Author information
Authors and Affiliations
Corresponding author
Rights and permissions
About this article
Cite this article
Yang, JH., Kim, Yl. & Kim, KM. Preparation and evaluation of aceclofenac microemulsion for transdermal delivery system. Arch Pharm Res 25, 534–540 (2002). https://doi.org/10.1007/BF02976614
Received:
Issue Date:
DOI: https://doi.org/10.1007/BF02976614