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Transungual Gel of Terbinafine Hydrochloride for the Management of Onychomycosis: Formulation, Optimization, and Evaluation

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Abstract

The present study was aimed to optimize, develop, and evaluate microemulsion and microemulsion-based gel as a vehicle for transungual drug delivery of terbinafine hydrochloride for the treatment of onychomycosis. D-optimal mixture experimental design was adopted to optimize the composition of microemulsion having amount of oil (X 1), Smix (mixture of surfactant and cosurfactant; X 2), and water (X 3) as the independent variables. The formulations were assessed for permeation (micrograms per square centimeter per hour; Y 1), particle size (nanometer; Y 2), and solubility of the drug in the formulation (milligrams per milliliter; Y 3). The microemulsion containing 3.05% oil, 24.98% Smix, and 71.96% water was selected as the optimized formulation. The microemulsion-based gel showed better penetration (∼5 folds) as well as more retention (∼9 fold) in the animal hoof as compared to the commercial cream. The techniques used to screen penetration enhancers (hydration enhancement factor, ATR-FTIR, SEM, and DSC) revealed the synergistic effect of combination of urea and n-acetyl cysteine in disruption of the structure of hoof and hence, leading to enhanced penetration of drug.

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ACKNOWLEDGEMENTS

The authors would like to thank Indian Council of Medical Research (ICMR), New Delhi (Grant No. 45/71/2013/PHA/BMS) for the financial support.

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  1. Pharmaceutics Division, Department of Pharmaceutical Sciences, Punjabi University, Patiala, India

    Purva Thatai & Bharti Sapra

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  1. Purva Thatai
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Correspondence to Bharti Sapra.

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Thatai, P., Sapra, B. Transungual Gel of Terbinafine Hydrochloride for the Management of Onychomycosis: Formulation, Optimization, and Evaluation. AAPS PharmSciTech 18, 2316–2328 (2017). https://doi.org/10.1208/s12249-017-0711-7

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  • DOI: https://doi.org/10.1208/s12249-017-0711-7

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