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Preparation and physicochemical characterization of ketoprofen-loaded emulsions

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Abstract

The objective of this study was to prepare ketoprofen-loaded emulsions. The emulsions were formulated by mixing soybean oil, surfactants (a mixture of Tween 20 and Tween 80), and distilled water. To determine the most suitable composition for the emulsions, a phase diagram was drawn, representing a mixture of soybean oil, surfactants, and distilled water. From the phase diagram, one-phase formulations were selected and the particle sizes of the formulations were compared. The stability of each formulation was confirmed over 4 weeks at 4 °C, by looking for any change in particle size. The effect of dilution on the pH of emulsion formulations was recorded. A soybean oil concentration of 5 % was sufficient to obtain emulsions. The surfactants used were a mixture of Tween 20 and Tween 80 in a 1:2 ratio, to ensure high ketoprofen solubility. Three formulations, termed E1, E2, and E3, produced emulsions with relatively small particles. The ketoprofen-loaded E1 formulation resulted in the smallest particles. The three formulations were physically stable for 4 weeks with no significant change in particle size. Dilution with distilled water did not alter the pH of the three emulsion formulations, but did change the conductivity. In conclusion, ketoprofen was solubilized by the emulsion formulation, and then remained stable when maintained at 4 °C; additionally, while the pH was unaltered, the conductivity of the formulation was changed by dilution with distilled water.

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References

  • Ahmad N, Ramsch R, Llinàs M, Solans C, Hshim R, Tajuddin HA (2014) Influence of nonionic branched-chain glycosides on a model nano-emulsion for drug delivery systems. Colloids Surf B Biointeraces 115:267–274

    Article  CAS  Google Scholar 

  • Araya H, Tomita M, Hayashi M (2005) The novel formulation design of O/W microemulsion for improving the gastrointestinal absorption of poorly water soluble compounds. Int J Pharm 305:61–74

    Article  CAS  PubMed  Google Scholar 

  • Bassani AS, Banov D, Phan H (2016) Characterization of the percutaneous absorption of ketoprofen using the Franz skin finite dose model. Postgrad Med 128:262–267

    Article  PubMed  Google Scholar 

  • Cerciello A, Auriemma G, Morello S, Pinto A, Del Gaudio P, Russo P, Aquino RP (2015) Design and in vivo anti-inflammatory effect of ketoprofen delayed delivery systems. J Pharm Sci 104(10):3451–3458

    Article  CAS  PubMed  Google Scholar 

  • Chatzidaki MD, Arik N, Monteil J, Papadimitriou V, Leal-Calderon F, Xenakis A (2016) Microemulsion versus emulsion as effective carrier of hydroxytyrosol. Colloids Surf B Biointerfaces 137:146–151

    Article  CAS  PubMed  Google Scholar 

  • Cho YD, Park YJ (2014) In vitro and in vivo evaluation of a self-microemulsifying drug delivery system for the poorly soluble drug fenofibrate. Arch Pharm Res 37:193–203

    Article  CAS  PubMed  Google Scholar 

  • Derry S, Moore RA, Gaskell H, McIntyre M, Wiffen PJ (2015) Topical NSAIDs for acute musculoskeletal pain in adults. Cochrane Database Syst Rev 6:CD007402

    PubMed  Google Scholar 

  • Drug Bank database. Drug card for ketoprofen. http://www.drugbank.ca/drugs/DB01009. Accessed 29 Feb 2016

  • Gangishetty H, Eedara BB, Bandari S (2015) Development of ketoprofen loaded proliposomal powders for improved gastric absorption and gastric tolerance: in vitro and in situ evaluation. Pharm Dev Technol 26:641–651

    Article  Google Scholar 

  • Gao ZG, Choi HG, Shin HJ, Park KM, Lim SJ, Hwang KJ, Kim CK (1998) Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosporin A. Int J Pharm 161:75–85

    Article  CAS  Google Scholar 

  • Gonçalves VSS, Rodríguez-Rojo S, Matias AA, Nunes AVM, Nogueira ID, Nunes D, Fortunato E, Alves de Matos AP, Cocero MJ, Duarte CMM (2015) Development of multicore hybrid particles for drug delivery through the precipitation of CO2 saturated emulsions. Int J Pharm 478:9–18

    Article  PubMed  Google Scholar 

  • Groves MJ, de Galidez DA (1976) The self-emulsifying action of mixed surfactants in oil. Acta Pharm Suec. 13:361–372

    CAS  PubMed  Google Scholar 

  • Gürol Z, Hekimoglu S, Demirdamar R, Sumnu M (1996) Percutaneous absorption of ketoprofen. I. In vitro release and percutaneous absorption of ketoprofen from different ointment bases. Acta Helv. 71:205–212

    Article  Google Scholar 

  • Kalaitzaki A, Poulopoulou M, Papadimitrou V, Xenakis A (2014) Surfactant-rich biocompatible miroemulsions as effective carriers of methylxanthin drugs. Colloids Surf A 442:80–87

    Article  CAS  Google Scholar 

  • Khan IU, Serra CA, Anton N, Er-Rafik M, Blanck C, Schmutz M, Kraus I, Messaddeq N, Sutter C, Anton H, Klymchenko AS, Vandamme TF (2015) Microfluidic conceived Trojan microcarriers for oral delivery of nanoparticles. Int J Pharm 493(1–2):7–15

    Article  CAS  PubMed  Google Scholar 

  • Kumar R, Sinha VR (2014) Preparation and optimization of voriconazole microemulsion for ocular delivery. Colloids Surf B: Biointerfaces 117:82–88

    Article  CAS  PubMed  Google Scholar 

  • Kytariolos J, Charkoftaki G, Smith JR, Voyiatzis G, Chrissanthopoulos A, Yannopoulos SN, Fatouros DG, Macheras P (2013) Stability and physicochemical characterization of novel milk-based oral formulations. Int J Pharm 444:128–138

    Article  CAS  PubMed  Google Scholar 

  • Lodén M, Åkerström U, Lindahl K, Berne B (2004) Bioequivalence determination of topical ketoprofen using a dermatophamacokinetic approach and excised skin penetration. Int J Pharm 284:23–30

    Article  PubMed  Google Scholar 

  • Lorier M, Magallanes L, Ibarra M, Guevara N, Vázquez M, Fagiolino P (2015) Stereoselective pharmacokinetics of ketoprofen after oral administration of modified-release formulations in Caucasian healthy subjects. Eur J Drug Metab Pharmaclokinet. doi:10.1007/s13318-015-0313-2

  • Podlogar F, Bešter Rogač M, Gašperlin M (2005) The effect of internal structure of selected water-Tween 40®-Imwitor 308®-IPM microemulsions on ketoprofen release. Int J Pharm 302:68–77

    Article  CAS  PubMed  Google Scholar 

  • Shohin IE, Kulinich JI, Ramenskaya GV, Abrahamsson B, Kopp S, Langguth P, Polli JE, Shah VP, Grroy DW, Barends DM, Dressman JB (2012) Biowaiver monographs for immediate-release solid oral dosage forms: ketoprofen. J Pharm Sci 101:3593–3603

    Article  CAS  PubMed  Google Scholar 

  • Siqueira J, Smiley D, Newton C, Le NA, Gosmanov AR, Spiegelman R, Peng L, Osteen SJ, Jones DP, Quyyumi AA, Ziegler TR, Umpierrez GE (2011) Substitution of standard soybean oil with olive oil-based lipid emulsion in parenteral nutrition: comparison of vascular, metabolic, and inflammatory effects. J Clin Endocrinol Metab 96:3207–3216

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Tartau L, Cazacu A, Melnig V (2012) Ketoprofen-liposomes formulation for clinical therapy. J Mat Sci Mar Med. 23:2499–2507

    Article  CAS  Google Scholar 

  • Uchino T, Lefeber F, Gooris G, Bouwstra J (2014) Characterization and skin permeation of ketoprofen-loaded vesicular systems. Eur J Pharm Biopharm 86:156–166

    Article  CAS  PubMed  Google Scholar 

  • Yalkowsky SH, Dannenfelser RM (1992) The aquasol database of aqueous solubility. College of Pharmacy, University of Arizona, Tucson

    Google Scholar 

  • Zhang J, Michniak-Kohn B (2011) Investigation of microemulsion microstructures and their relationship to transdermal permeation of model drugs: ketoprofen, lidocaine, and caffeine. Int J Pharm 421:34–44

    Article  CAS  PubMed  Google Scholar 

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Acknowledgments

This article does not contain any studies with human and animal subjects performed by any of the authors. And all authors (S Park, SE Lee, JK Lee, TH Kim, WS Jang and JS Park) declare that they report no conflict of interest. This work was supported by research fund of Chungnam National University in 2015.

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Correspondence to Jeong-Sook Park.

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Saeul Park and Sang-Eun Lee have contributed equally to this work.

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Park, S., Lee, SE., Lee, JK. et al. Preparation and physicochemical characterization of ketoprofen-loaded emulsions. Journal of Pharmaceutical Investigation 46, 487–493 (2016). https://doi.org/10.1007/s40005-016-0247-y

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