Formulation and evaluation of croconazol hydrochloride topical gels

ABSTRACT

This study was designed to evaluate different polymers for their suitability as a vehicles for topical drug delivery systems. Croconazol hydrochloride is an azol derivative used as antimycotic agent. It was incorporated in this vehicles as a gel forms in a concentration of 1.0% w/w. Polymers used in this study are methylcellulose [MC], Tylose [Ty], Polyvinyl alcohol [PVA,], Pluronic F-127 [pl. F-127], Polyethylene glycol [PEG], Carbopol 974P [Carb.] and Eudispert mv. [Eud]. They were used in a suitable concentration for gel formulation. In-vitro release characteristics of the drug from different gels were carried out using dialysis membrane in phosphate buffer pH 5.2. The release data were treated with various kinetic principles to assess the relevant parameters. The general rank order of Croconazol hydrochloride release from the prepared gel were MC > Ty > pl. F-127 > PVA > Carb > Eud > PEG. The results showed that, the release of drug from the prepared gels obeyed the diffusion model [Higuchi's equation]. Some kinetic parameters were calculated such as diffusion coefficient, permeability coefficient and the partition coefficient. The results indicated a direct dependence of the release rate on the diffusion coefficient. The influence of initial drug concentration [0.5, 1.0 and 2.0% w/w], and p1 F-127 concentratio,2 [20, 25, 30% w/w] on the release patterns was studied The obtained data revealed an inverse correlation between the drug release rate and the pluronic F-127 concentration and a direct correlation between the drug release rate and the initial drug concentration. The anti-fungal activity of the different gel formulations was evaluated by agar-cup plate technique using five fungal species. The results obtained indicated that, all gel formulations have good anti-fungal activities