Solubilization of fluocinolone acetonide by cosolvents and surfactants for buccal solution preparation

Pornpen Werawatganone, Walaisiri Muangsiri, Tipanan Chaivanon, Pavinee Kungwanpongpun, Paricha Rattanawong

Abstract


Fluocinolone acetonide (FA) buccal solution was prepared for treatment of oral lichen planus using cosolvents and surfactant to enhance FA solubility. Based on solubility power (s), cosolvents enhanced FA solubility in the order; polyethylene glycol 400 (s=3.06×10-2) > propylene glycol (s=2.92×10-2) > glycerin (s=0.95×10-2). The order of FA solubility in surfactant solutions was 1% polysorbate 80 (1.04×10-2 %w/v) > 0.05% cetypyridinium chloride (0.69×10-2 %w/v) > 0.1% sodium lauryl sulfate (0.27×10-2 %w/v). Cosolvents increased the critical micelle concentration (CMC), especially for ionizable surfactants (sodium lauryl sulfate and cetylpyridinium chloride). This influence of cosolvents on micellization impeded the ability of the surfactants to increase FA solubility. Both polysorbate 80 and cetylpyridinium chloride induced instability of FA. We conclude that a 0.01% FA buccal solution should be prepared in a cosolvent system without use of surfactants.


Full Text:

84-89;PDF

References


Buajeeb W, Pobrurksa C, Kraivaphan P. Efficacy of fluocinolone acetonide gel in the treatment of oral lichen planus. Oral Surg Oral Med Oral Pathol Oral Radiol and Endod 2000; 89: 42-45.

Thongprasom K, Luengvisut P, Wongwatanakij A, Boonjatturus C. Clinical evaluation in treatment of oral lichen planus with topical fluocinolone acetonide: a 2-year follow-up. J Oral Pathol Med 2003; 32: 315-322.

Davari P, Hsiao H-H, Fazel N. Mucosal Lichen Planus: An Evidence-Based Treatment Update. Am J Clin Dermatol 2014; 15: 181-195.

Setterfield J F, Black M M, Challacombe S J. The management of oral lichen planus. Clin Exp Dermatol 2000; 25: 176-182.

Brayfielf A. editor, Martindale : the complete drug reference. 38 ed., Pharmaceutical Press; 2014, 1636.

Gao H Y, Po A L W. Topical formulations of fluocinolone acetonide - are creams, gels and ointments bioequivalent and does dilution affect activity. Eur J Clin Pharmacol 1994; 46: 71-75.

Gonzalez-Garcia A, Diniz-Freitas M, Gandara-Vila P, Blanco-Carrion A, Garcia-Garcia A, Gandara-Rey J M. Triamcinolone acetonide mouth rinses for treatment of erosive oral lichen planus: efficacy and risk of fungal over-infection. Oral Dis 2006; 12: 559-565.

Jainkittivong A, Kuvatanasuchati J, Pipattanagovit P, Sinheng W. Candida in oral lichen planus patients undergoing topical steroid therapy. Oral Surg Oral Med Oral Pathol Oral Radiol and Endod 2007; 104: 61-66.

British Pharmacopoeia Commission. British Pharmacopoeia. The Stationery Office on behalf of the Medicines and Helthcare products Regulatory Agency (MHRA), London, UK, 2013, 947-948.

Kenley R A, Lee M O, Sukumar L, Powell M F. Temperature and ph dependence of fluocinolone acetonide degradation in a topical cream formulation. Pharm Res 1987; 4: 6.

Ruelle P, Farina-Cuendet A, Kesselring U W. Hydrophobic and solvation effects on the solubility of hydroxysteroids in various solvents: Quantitative and qualitative assessment by application of the mobile order and disorder theory. Perspect Drug Discov 2000; 18: 52.

Yalkowsky S H. Solubility and Solubilizatoin in Aqueous Media. Oxford University Press, Inc., 1999, 180-320.

Ran Y, Zhao L, Xu Q, Yalkowsky S H. Solubilization of Cyclosporin A. AAPS PharmSciTech 2: 4.

Raymond R C, Sheskey P J, Cook W G, Fenton M E. Handbook of Pharmaceutical Exicipients. 7 th ed., Pharmaceutical Press, London, UK, 2012.

Dai S, Tam K C. Effect of cosolvents on the binding interaction between poly(ethylene oxide) and sodium dodecyl sulfate. J Phys Chem B 2006; 110: 20794-20800.

Rosen M J. Micelle Formation by Surfactants. In: Rosen M. J., (ed) Surfactants and Interfacial Phenomena. 3 rd ed., John Wiley & Sons, Inc., New Jersy, 2004; 105-177.

Hansch C L, Albert ; Hoekman D H Exploring QSAR. Washington, DC: American Chemical Society, 1995.

Baert J H, Veys R J, Ampe K, DeBoever J A. The effect of sodium lauryl sulphate and triclosan on hamster cheek pouch mucose. Int J Exp Pathol 1996; 77: 73-78.

De Jongh C M, Lutter R, Verberk M M, Kezic S. Differential cytokine expression in skin after single and repeated irritation by sodium lauryl sulphate. Exp Dermatol 2007; 16: 1032-1040.

Gloor M, Senger B, Langenauer M, Fluhr J W. On the course of the irritant reaction after irritation with sodium lauryl sulphate. Skin Res Technol 2004; 10: 144-148.

Pirot F, Panisset F, Agache P, Kalia Y N, Humbert P. Comparison of four, non-invasive, quantitative probes of skin irritation induced by sodium lauryl sulphate. Eur J Derm 1995; 5: 709-714.

Shim Y J, Choi J H, Ahn H J, Kwon J S. Effect of sodium lauryl sulfate on recurrent aphthous stomatitis: a randomized controlled clinical trial. Oral Dis 2012; 18: 655-660.

Brokstad B, Barkvoll P. The effect of two toothpaste detergents on the frequency of recurrent aphthous ulcers. Acta Odontol Scand 1996; 54: 150-153.

Herlofson B B, Barkvoll P. Sodium lauryl sulfate and recurrent aphthous ulcers - a preliminary-study. Acta Odontol Scand 1994; 52: 257-259.


Refbacks

  • There are currently no refbacks.