Bigels with antifungal substances, ciclopirox olamine and terbinafine hydrochloride, were made of hydrogel (poloxamer 407 gel) and oleogel (polyethylene and liquid paraffin mixture). Prepared bigels were found physically stable at room temperature for six months and at least four months at 40 °C. Released amount of drug decreased when oleogel concentration in the formulation increased. Release test results depended on the insertion place of active substances. The amount of released substance was highest when ciclopirox olamine was incorporated in both phases in an equal quantity, and terbinafine hydrochloride in oleogel or in hydrogel. All formulations showed great inhibition of Microsporum canis. Thus, bigels with ciclopirox olamine and terbinafine hydrochloride are a promising dosage form for topical use.
1. Y. C. Chen, D. Z. Liu, J. J. Liu, T. W. Chang, H. O. Ho and M. T. Sheu, Development of terbinafine solid lipid nanoparticles as a topical delivery system, Int. J. Nanomedicine 7 (2012) 4409–4418; https://doi.org/10.2147/IJN.S33682
2. I. F. Almeida, A. R. Fernandes, L. Fernandes, M. R. Pena Ferreira, P. C. Costa and M. F. Bahia, Moisturizing effect of oleogel/hydrogel mixtures, Pharm. Dev. Technol. 13 (2008) 487–494; https://doi.org/10.1080/10837450802282447
3. S. Bangarwa, S. Garg and A. Aseri, A review on antifungal gels: as a topical drug delivery system, Int. J. Pharm. Technol. Biotechnol. 1 (2014) 48–55.
4. V. K. Singh, I. Banerjee, T. Agarwal, K. Pramanik, M. K. Bhattacharya and K. Pal, Guar gum and sesame oil based novel bigels for controlled drug delivery, Colloids Surfaces B Biointerfaces 123 (2014) 582–592; https://doi.org/10.1016/j.colsurfb.2014.09.056
5. F. R. Lupi, L. Gentile, D. Gabriele, S. Mazzulla, N. Baldino and B. de Cindio, Olive oil and hyperthermal water bigels for cosmetic uses, J. Colloid Interface Sci. 459 (2015) 70–78; https://doi.org/10.1016/j.jcis.2015.08.013
6. M. J. Dolton, V. Perera, L. G. Pont and A. J. McLachlan, Terbinafine in combination with other antifungal agents for treatment of resistant or refractory mycoses: investigating optimal dosing regimens using a physiologically based pharmacokinetic model, Antimicrob. Agents Chemother. 58 (2014) 48–54; https://doi.org/10.1128/AAC.01466-13
7. M. K. Kathiravan, A. B. Salake, A. S. Chothe, P. B. Dudhe, R. P. Watode, M. S. Mukta, S. Gadhwe, The biology and chemistry of antifungal agents: A review, Bioorg. Med Chem. 20 (2012) 5678–5698; https://doi.org/10.1016/j.bmc.2012.04.045
8. K. Tabara, A. E. Szewczyk, W. Bienias, A. Wojciechowska, M. Pastuszka, M. Oszukowska, A. Kaszuba, Amorolfine vs. ciclopirox – Lacquers for the treatment of onychomycosis, Postep. Dermatol. Alergol. 32 (2015) 40–45; https://doi.org/10.5114/pdia.2014.40968
9. A. Mazurkeviciute, K. Ramanauskiene, M. Ivaskiene, A. Grigonis and V. Briedis, Modelling and biopharmaceutical evaluation of ciclopirox olamine gels, Acta Pol. Pharm. 74 (2017) 543–549.
10. J. Ma, Y. Lin, X. Chen, B. Zhao and J. Zhang, Flow behavior, thixotropy and dynamical viscoelasticity of sodium alginate aqueous solutions, Food Hydrocoll. 38 (2014) 119–128; https://doi.org/10.1016/j.foodhyd.2013.11.016
11. M. T. Islam, N. Rodriguez-Hornedo, S. Ciotti and C. Ackermann, Rheological characterization of topical carbomer gels neutralized to different pH, Pharm. Res. 21 (2004) 1192–1199; https://doi.org/10.1023/B:PHAM.0000033006.11619.07
12. M. M. Ibrahim, S. A. Hafez and M. M. Mahdy, Organogels, hydrogels and bigels as transdermal delivery systems for diltiazem HCL, Asian J. Pharm. Sci. 8 (2013) 46–54; https://doi.org/10.1016/j.ajps.2013.07.006
13. A. Kaur, S. Jaiswal and G. D. Gupta, Formulation and evalution of terbinafine hydrochloride topical gel, Indo. Am. J. Pharm. Res. 4 (2014) 2919–2927.
14. M. E. Herbig and D. H. Evers, Correlation of hydrotropic solubilization by urea with log D of drug molecules and utilization of this effect for topical formulations, Eur. J. Pharm. Biopharm. 85 (2013) 158–160; https://doi.org/10.1016/j.ejpb.2013.06.022
15. J. Leyden, Pharmacokinetics and pharmacology of terbinafine and itraconazole, J. Am. Acad. Dermatol. 38 (1998) 42–47; https://doi.org/10.1016/S0190-9622(98)70483-9