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Formulation development and optimization of transungual drug delivery system of terbinafine hydrochloride for the treatment of onychomycosis

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Abstract

The aim of present investigation was to develop transungual drug delivery system (nail lacquer) of terbinafine hydrochloride for treatment of onychomycosis. Different types of penetration enhancers, viz. 2-mercaptoethanol, n-acetyl-l-cysteine and thioglycolic acid, were evaluated to determine their effect on drug permeation. Various types of polymers, both hydrophobic (Eudragit® RL 100 and Eudragit® RS 100) and hydrophilic polymers (hydroxypropyl methyl cellulose (HPMC) E15), were evaluated for their film-forming and drug permeation characteristics. The nail lacquer was optimised statistically by applying 32 full factorial design. Polymer ratio (Eudragit® RL 100/HPMC E15; X 1) and solvent ratio (ethanol/water; X 2) were selected as independent variable, and viscosity (cPs), nail plate hydration (%) and in vitro drug permeated at the end of 24 h (μg/cm2) were selected as dependent variable. The optimised batch comprises of polymer ratio (70:30) and solvent ratio (75:25). Ex vivo drug permeation study was performed using human cadaver toe nail plate. The results revealed that the amount of drug permeated at the end of 24 h was 61.55 ± 3.2 μg/cm2, which was found to be higher than the minimum inhibitory concentration of drug. This study confirms that the developed drug-loaded nail lacquer could be used as a promising tool for the effective treatment of onychomycosis.

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Authors and Affiliations

  1. Department of Pharmaceutics, Institute of Pharmacy, Nirma University, SG Highway, Chharodi, Ahmedabad, 382481, Gujarat, India

    Mayur M. Patel & Zeal M. Vora

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  1. Mayur M. Patel
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  2. Zeal M. Vora
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Correspondence to Mayur M. Patel.

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Patel, M.M., Vora, Z.M. Formulation development and optimization of transungual drug delivery system of terbinafine hydrochloride for the treatment of onychomycosis. Drug Deliv. and Transl. Res. 6, 263–275 (2016). https://doi.org/10.1007/s13346-016-0287-x

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