Abstract
The aim of the present investigation was to evaluate microemulsion as a vehicle for dermal drug delivery and to develop microemulsion-based gel of terbinafine for the treatment of onychomycosis. D-optimal mixture experimental design was adopted to optimize the amount of oil (X 1), Smix (mixture of surfactant and cosurfactant; X 2) and water (X 3) in the microemulsion. The formulations were assessed for globule size (in nanometers; Y 1) and solubility of drug in microemulsion (in milligrams per milliliter; Y 2). The microemulsion containing 5.75% oil, 53.75% surfactant–cosurfactant mixture and 40.5% water was selected as the optimized batch. The globule size and solubility of the optimized batch were 18.14 nm and 43.71 mg/ml, respectively. Transmission electron microscopy showed that globules were spherical in shape. Drug containing microemulsion was converted into gel employing 0.75% w/w carbopol 934P. The optimized gel showed better penetration and retention in the human cadaver skin as compared to the commercial cream. The cumulative amount of terbinafine permeated after 12 h was 244.65 ± 18.43 μg cm−2 which was three times more than the selected commercial cream. Terbinafine microemulsion in the gel form showed better activity against Candida albicans and Trichophyton rubrum than the commercial cream. It was concluded that drug-loaded gel could be a promising formulation for effective treatment of onychomycosis.
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Acknowledgments
The authors are thankful to Cadila Pharmaceuticals Ltd. (Ahmedabad, India) for providing terbinafine; Abitec Corporation (OH, USA) for providing Capmul MCM; and Gattefosse (Lyon, France) for providing the free samples of Labrasol, Labrafac, and Transcutol P. The authors are also thankful to Institute of Microbial Technology (Chandigarh, India) for providing the fungal strains. The authors are grateful to Mrs. Mallika Babu for proof-reading the manuscript for grammatical and spelling errors. This study is a part of research project, carried out at Kadi Sarva Vishwavidyalaya (Gandhinagar, India).
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Barot, B.S., Parejiya, P.B., Patel, H.K. et al. Microemulsion-Based Gel of Terbinafine for the Treatment of Onychomycosis: Optimization of Formulation Using D-Optimal Design. AAPS PharmSciTech 13, 184–192 (2012). https://doi.org/10.1208/s12249-011-9742-7
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DOI: https://doi.org/10.1208/s12249-011-9742-7