FORMULATION AND EVALUATION OF CANDESARTAN CILEXETIL TRANSDERMAL PRONIOSOMAL GEL

Abstract

The present work deals with the preparation of candesartan cilexetil proniosomal gel by coaservation phase separation method by using different surfactants, cholesterol and soya lecithin in 9:1:9 and 9:2:9 ratios. The prepared proniosomal gel formulations were evaluated for vesicle size analysis, surface morphological studies, encapsulation efficiency, In vitro drug release, ex vivo skin permeation studies and vesicular stability at different storage conditions. The results showed that candesartan cilexetil in all the formulations was successfully entrapped and a substantial change in release rate and an alteration in the encapsulation efficiency of candesartan cilexetil from proniosomes were observed upon varying the type of surfactant and cholesterol content. Vesicles formed with Spans were  smaller in size than vesicles formed with Tweens. Encapsulation efficiency of proniosomes formed from Span 60, Span 40, Span20, and Span 80 was found high compared with proniosomes prepared from Tweens (Tween 20 and Tween 80). An optimised preparation with 9:2:9 ratio of Span 60, cholesterol and lecithin gave maximum encapsulation efficiency (92.29%) and showed drug release (95.89±0.26%) in a controlled manner with a flux value of 1.89 μg/cm² /hr and permeability co efficient value of 0.094 cm²/hr as compared to other compositions. No significant changes in relation to vesicle size and encapsulation efficiency were recorded after stability studies. It is evident from this study that proniosomes are a promising prolonged delivery system for candesartan cilexetil and have reasonably good stability characteristics.

Keywords: candesartan cilexetil, proniosomes, encapsulation efficiency, flux, stability.