Formulation and Evaluation of Proniosome Based Drug Delivery System of the Antifungal Drug Clotrimazole

Abstract

In the present study proniosomal gel of clotrimazole was formulated by using lecithin, cholesterol as encapsulating agents, nonionic surfactants Span and Tween with different grades. Evaluation of proniosomal gels for pH, vesicle size analysis, encapsulation efficiency, drug diffusion profiles, ex-vivo skin permeation and ex-vivo drug deposition studies on guinea pig skin, irritation test on rabbit and stability studies was performed. The preliminary compatibility studies revealed that there were no interactions between clotrimazole and excipients which was evident from FTIR and DSC studies. The physical characteristics of proniosomal gels were found to be within the acceptable limits. The vesicle size was found to be in the range 5.25-15.23μm. The proniosomes were spherical and homogenous in structure when observed under optical microscopy. The ex-vivo skin permeation and ex-vivo drug deposition studies showed the drug release from formulations F3, F4 and marketed formulation was 48.60%, 36.9% and 27.48 % respectively and the percent of clotrimazole deposited in skin after 24 h was found to be 35.7%, 43.6% and 15.17% for formulation F3, F4 and marketed formulation respectively. The release from the proniosomal gel was prolonged when compared to conventional formulation and showed a two fold increase in the drug deposition in the skin compared to conventional cream. No obvious erythema, edema or inflammation was observed on rabbits’ skin after one week of application of the selected formulation. Results of antifungal studies revealed that the developed proniosomal gel is more efficient when compared with the marketed formulation. The stability studies showed that proniosomal gels were stable at 5±3°C and 25±2°C. The above results indicated that the proniosomal gels of clotrimazole could be formulated for sustained release.