Stability determination of an alternative approach to use of liquid drug substance as oil phase in microemulsion formulations: methyl salicylate
Abstract
The objective of this study was to investigate the stability of microemulsions using methyl salicylate as oil phase in the presence and the absence of hydrophobic additives and/or drug after six-month storage at ambient temperature. The investigated additives were menthol, isopropyl palmitate and isopropyl myristate. Indomethacin was as a model drug. The surfactant system of Tween 20-isopropyl alcohol (1:1) was kept constant at 50% while the dispersed phase was at 15% in which weight ratios of methyl salicylate to additive were varied. Formulations were prepared and then characterized. All samples were transparent homogenous liquids with nano-sized droplets and the O/W characteristic. After storage, all samples visually remained unchanged. The analytical results showed methyl salicylate and indomethacin were stable in the prepared microemulsions. The optimized oil phase comprised menthol as additive at a 3:1 weight ratio of methyl salicylate to menthol in the presence and the absence of indomethacin.
Full Text:
157-165;PDFReferences
References
Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliver Rev 2000;45:89-121.
Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliver Rev 2012;64:175-193.
Attwood D. Microemulsions. In: Kreuter J, editor. Colloidal Drug Dlivery Systems. New York: Maecel Dekker; 2004, p. 31-65.
Paolino D, Ventura CA, Nistico S, et al. Lecithin microemulsions for the topical administration of ketoprofen: percutaneous adsorption through human skin and in vivo human skin tolerability. Int J Pharm 2002;244:21-31.
Nandi I, Bari M, Joshi H. Study of isopropyl myristatemicroemulsion systems containing cyclodextrins to improve the solubility of 2 model hydrophobic drugs. AAPS PharmSciTech 2003;4:71-79.
El Maghraby GM. Transdermal delivery of hydrocortisone from eucalyptus oil microemulsion: Effects of cosurfactants. Int J Pharm 2008;355:285-292.
Raza K, Negi P, Takyar S, et al. Novel dithranol phospholipid microemulsion for topical application: development, characterization and percutaneous absorption studies. J Microencapsul 2011;28:190-199.
Fanun M. Microemulsions as delivery systems. Curr Opin Colloid In, 2012;17:306-313.
El Maghraby GM, Arafa MF, Osman MA. Microemulsion for simultaneous transdermal delivery of benzocaine and indomethacin: in vitro and in vivo evaluation. Drug Dev Ind Pharm 2014;40:1637-1644.
Negi P, Singh B, Sharma G, et al. Phospholipid microemulsion-based hydrogel for enhanced topical delivery of lidocaine and prilocaine: QbD-based development and evaluation. Drug Deliv 2016; 23:941-957.
Sharma G, Dhankar G, Thakur K, et al. Benzyl benzoate-loaded microemulsion for topical applications: Enhanced dermatokinetic profile and better delivery promises. AAPS PharmSciTech 2016;17: 1221-1231.
Kogan A, Garti N. Microemulsions as transdermal drug delivery vehicles. Adv Colloid Interfac 2006;123–126:369-385.
Sato K, Sugibayashi K, Morimoto Y. Effect and mode of action of aliphatic esters on the in vitro skin permeation of nicorandil. Int J Pharm 1988;43:31-40.
Walker RB, Smith EW. The role of percutaneous penetration enhancers. Adv Drug Deliv Rev 1996;18:295-301.
Kunta JR, Goskonda VR, Brotherton HO, et al. Effect of menthol and related terpenes on thepercutaneous absorption of propranolol across excised hairless mouse skin. J Pharm Sci 1997;86:1369-1373.
Guo H, Liu Z, Li J, et al. Effects of isopropyl palmitate on the skin permeation of drugs. Biol Pharm Bull 2006;29:2324-2326.
Leesajakul W, Taworn C, Channarong S. Methyl salicylate microemulsion-based systems. Part I: Effect of additives on the physicochemical properties. Int J Pharm Pharm Sci 2014;6:137-141.
O’Neil MJ. The Merck Index: An encyclopedia of chemicals drugs, and biological. 15th ed. Cambridge: The Royal Society of Chemistry; 2013.
Brayfield A. Martindale: The complete drug reference. 38th ed. London: Pharmaceutical Press; 2014.
Chen H, Chang X, Du D, Li J, Xu H, Yang X. Microemulsion-based hydrogel formulation of ibuprofen for topical delivery. Int J Pharm 2006;315:52-58.
Friberg SE. Micelies, microemulsions, liquidcrystals, and the structure of stratum corneum lipids. J Soc Cosmet Chem 1990;41:155-171.
Müller-Goymann, CC. Physicochemical characterization of colloidal drug delivery systems such as reverse micelles, vesicles, liquid crystals and nanoparticles for topical administration. Eur J Pharm Biopharm 2004;58:343-356.
Alany RG, Tucker IG, Davies NM, Rades T. Characterizing colloidal structures of Pseudoternary Phase Diagrams Formed by Oil/Water/Amphiphile Systems. Drug Dev Ind Pharm 2001;27:31–38.
Djordjevic L, Primorac M, Stupar M. In vitro release of diclofenac diethylamine from caprylocaproyl macrogol glycerides based microemulsions. Int J Pharm 2005;296:73-79.
Alany RG, Wen J. Microemulsions as drug delivery systems. In: Gad SC, editor. Pharmaceutical manufacturing handbook: production and processes. New Jersey: John Wiley & Sons; 2008, p.769-792.
Baroli B, López-Quintela MA, Delgado-Charro MB, et al. Microemulsions for topical delivery of 8-methoxsalen. J Control Release 2000;69:209-218.
Richardson CJ, Mbanefo A, Aboofazeli R, et al. Prediction of Phase Behavior in Microemulsion Systems Using Artificial Neural Networks. J Colloid Interf Sci 1997;187:296-303.
Park KM, Kim CK. Preparation and evaluation of flurbiprofen-loaded microemulsion for parenteral delivery. Int J Pharm 1999;181:173-179.
Narang AS, Delmarre D, Gao D. Stable drug encapsulation in micelles and microemulsions. Int J Pharm 2007;345:9-25.
O’Brien M, McCauley J, Cohen E. Indomethacin. In: Florey K, editor. Analytical profiles of drug substances. vol 13. Orlando: Academic Press; 1984.
Trissel LA. Trissel’sTM stability of compounded formulations. 5th ed. Washington, DC: American Pharmacists Association; 2012.
Khan MN, Olagbemiro TO. Kinetic evidence for the occurrence of the oxydianionic tetrahedral intermediates in the hydrolyses of methyl salicylate and methyl o-methoxybenzoate in a highly alkaline medium. J Org Chem 1982;47:3695-3699.
Khan MN. Effects of anionic micelles on the intramolecular general base-catalyzed hydrolysis of phenyl and methyl salicylates. J Mol Catal A-Chem 1995;102:93-101.
Khan MN, Arifin Z. Effects of cationic micelles on rates and activation parameters of intramolecular general base-catalyzed hydrolysis of ionized salicylate esters. J Colloid Interf Sci 1996;180:9-14.
Stahl PH, Wermuth CG. Handbook of pharmaceutical salts: properties, selection, and use. 2nd ed. Zurich: Verlag Helvetica Chimica Acta; 2011.
Connors KA, Amidon GL, Stella VJ. Chemical Stability of Pharmaceuticals: A Handbook for Pharmacists. 2nd ed. New York: John Wiley and Sons; 1986.
Ghanem AH, El-Sabbagh H, Abdel-Alim H. Stability of indomethacin solubilized system. Pharmazie 1979;34:406-407.
Krasowska H. The hydrolysis of indomethacin in aqueous solutions of polysorbates. Int J Pharm 1979;4:89-97.
Vos AD, Vervoort L, Kinge R. Solubilization and stability of indomethacin in a transparent oil-water gel. Int J Pharm 1993;92:191-196.
Refbacks
- There are currently no refbacks.