Abstract

ENHANCED TRANSDERMAL DELIVERY OF KETOCONAZOLE VIA ETHOSOMES FORMULATION AND EVALUATION

*Shaik. Harun Rasheed¹, N.Tirumooorthy², Kundlik Girhepunje¹.

ABSTRACT

Ketoconazole is an antifungal drug useful in treatment of both dermatophytosis and systemic mycosis. However its oral administration is associated with number of demerits. The goal of the current investigation is to evaluate the transdermal potential of novel vesicular carrier, ethosomes, bearing ketoconazole an antifungal having limited transdermal permeation. ketoconazole loaded ethosomes were prepared, optimized and characterized for vesicular shape and surface morphology, vesicular size, size distribution, entrapment efficiency, vesicles skin interaction and stability. The ethosomal formulation (E9) having 3% phospholipids content and 40% ethanol showing the greatest entrapment (77.81±3.5%) and size range (169±9.4 nm) was selected for further transdermal permeation studies. An optimum polydispersity index (0.102±0.009) of ketoconazole loaded ethosomal formulation could better justify the homogeneous nature of the prepared ethosomal formulation Skin entrapment efficiency assessed by confocal laser scanning microscopy (CLSM) which revealed that enhanced permeation in the deeper layer of the skin (156 μm). Vesicle skin interaction study also showed that there was no interaction between the formulation and rat skin. Furthermore ethosomal delivery system could be considered for the treatment of number of dermal infections with better efficiency.

Keywords: Enhanced drug delivery, ethosomes, dermatophytosis, confocal laser scanning microscopy, systemic mycosis.