Novel jojoba oil-based emulsion gel formulations for clotrimazole delivery.

Jojoba oil-based emulgel formulations were prepared using different concentrations of various gelling agents, such as hydroxypropyl methylcellulose (HPMC) and Carbopol 934 P and combination of both. The prepared emulgels were physically evaluated for their stability after temperature cycle test, centrifugation and long-term shelf storage for 1 year at room temperature. The in vitro release at 37 °C was studied to define the effect of the concentration and type of the gelling agent. A comparison between the formulated emulgels and two commercially available products, Candistan® and Canesten® creams, was carried out to judge their efficacy and stability. The prepared emulgels exhibited non-Newtonian shear thinning behavior with little or no thixotropy. Four emulgels showed excellent stability as they demonstrated consistent rheological model under different treatment conditions. The in vitro release test showed variation in the extent of percent drug released. The drug release from the commercial preparation was lower than some of the prepared emulgel formulae. One formula containing combination of the two gelling agents (HPMC and Carbopol 934 P), showed excellent stability and high extent of clotrimazole release was microbiologically evaluated against Candida albicans using cylinder and plate method. The selected formula showed superior antimycotic activity compared to the commercially available formulation. Further in vivo animal studies for the obtained stable formula is recommended.

Optimized formulation for topical administration of clotrimazole using Pemulen polymeric emulsifier.

BACKGROUND: Emulgel topical formulation is a vehicle of potential for topical delivery of antifungal drugs. METHODS: The imidazole derivative antifungal drug, clotrimazole (CZ), was formulated into emulgels using two grades of hydrophobically modified co-polymers of acrylic acid, namely Pemulen TR1 and TR2. The prepared emulgels were evaluated for their rheological properties, short- and long-term stability, in vitro release at 37°C. Microbiological evaluation of the formula showed that optimum stability and release was carried out to measure its antifungal activity. RESULTS: All formulae showed non-Newtonian shear thinning behavior with little thixotropy or antithixotropy. Five of the prepared formulae showed good physical stability under different treatment conditions. Isopropyl myristate (IPM) emulgels exhibited higher rate of CZ release than either jojoba oil (JB) or liquid paraffin-based emulgels. A selected formula containing JB together with a combination of Pemulen TR1 and TR2 showed excellent stability as well as high rate of CZ release. Microbiological evaluation of the selected formula containing similar amount of CZ revealed 1.2-folds increase in the antifungal activity compared to commercially available formulation. CONCLUSION: Emulgel dosage form based on Pemulen polymeric emulsifier and JB is a promising vehicle for topical delivery of CZ and further in vivo animal studies are recommended.