In-vitro Evaluation of Transungual Formulation of Ketoconazole for the Management of Onychomycosis

Author(s): Purva Thatai, Karanjot Kaur, Bharti Sapra*.

Journal Name: Drug Delivery Letters

Volume 8 , Issue 2 , 2018

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Graphical Abstract:


Objective: The present study aims at optimizing, developing and evaluating the nail lacquer formulation for transungual delivery of ketoconazole for the management of onychomycosis.

Methodology: Nail lacquer (NL) of ketoconazole was formulated using two different types of polymers i.e. hydrophobic (Eudragit RL 100) and hydrophilic polymer (Klucel LF; hydroxyl-propyl cellulose). The optimization of NL was done statistically using 32 full factorial design. Different polymer ratios (Eudragit RL 100/ Klucel LF; X1) and solvent ratios (ethanol/water; X2) were selected as independent variables. The formulations were evaluated for drying time (sec; Y2), drug permeation (μg/cm2/h; Y1) and peak adhesive strength (PAS) of NL film (g; Y3). The optimized formulation was then characterized for various parameters (non-volatile content, blush test, manual in vitro measurement of film adhesion) and by utilizing different techniques like ATR-FTIR, DSC and SEM. Ex vivo activity of the optimized formulation was assessed against Candida albicans (MTCC No. 3018).

Results: The formulation having polymer ratio as 1:1 and solvent ratio as 90:10 was selected as the optimized formulation. The optimized NL formulation was observed to exhibit better penetration (~ 2.81 fold) as well as retention (~ 2.98 fold) in the animal hoof as compared to the marketed formulation. Ex vivo antifungal studies revealed that the antifungal activity of NL was ~1.25 fold greater than the marketed formulation and it further gets augmented in the presence of penetration enhancer.

Conclusion: The findings of the present study evinced the developed NL as a promising vehicle for transungual drug delivery.

Keywords: Transungual drug delivery, nail lacquer, ketoconazole, onychomycosis, azoles, benzofuran, allylamine.

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Article Details

Year: 2018
Page: [140 - 152]
Pages: 13
DOI: 10.2174/2210303108666180313141228
Price: $58

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