Purva Thatai, Karanjot Kaur and Bharti Sapra* Pages 140 - 152 ( 13 )
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.
Transungual drug delivery, nail lacquer, ketoconazole, onychomycosis, azoles, benzofuran, allylamine.
Department of Pharmaceutical Sciences, Pharmaceutics Division, Punjabi University, Patiala, Department of Pharmaceutical Sciences, Pharmaceutics Division, Punjabi University, Patiala, Department of Pharmaceutical Sciences, Pharmaceutics Division, Punjabi University, Patiala