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.