Formulation and Optimization of Clotrimazole-Loaded Proniosomal Gel Using 32 Factorial Design

Abstract

The main aim of the study was to develop and statistically optimize the proniosomal gel for enhanced transdermal delivery using 32 factorial designs to investigate the influence of both non-ionic surfactant and cholesterol to maximize the entrapment efficiency and flux. The concentration of non-ionic surfactant and cholesterol were taken as independent variables, while entrapment efficiency and flux were taken as dependent variables. The study showed that the entrapment efficiency depends on both cholesterol and surfactant, whereas permeation flux depends only on the surfactant. Proniosomal gel showed a significantly enhanced drug permeation through the skin, with an enhancement ratio 3.81±1.85 when compared to the drug solution. Comparative evaluation of permeation studies and the in vitro release study of optimized proniosomal gel (F5) with that of marketed gel and carbopol gel showed that the penetration of the optimized formulation was enhanced 1.75 times in comparison with that of the marketed formulation, and the release was in a controlled manner. Similarly, the anticandidial activity showed a significantly higher activity (p<0.05) than the marketed and carbopol gel. This may be due to the enhanced penetration of noisome-containing drug through the fungal cell wall, inhibiting the ergo sterol synthesis, thereby causing the fungal cell death due to the presence of penetration enhancer. The stability study at two different temperatures (30 ± 2°C and 4 ± 2°C) confirmed that the formulations were stable even at the end of 45 days. Hence, proniosomal gel is an efficient carrier for the delivery of clotrimazole, thereby prolonging the action.

Novel non-ionic surfactant proniosomes for transdermal delivery of lacidipine: optimization using 23factorial design andin vivoevaluation in rabbits

“…Second, the cholesterol will compete with the drug for the space within the bilayer, hence remove the drug from the vesicles bilayer (Wang et al, 2010;Abdelbary, 2011). These results fit well with previously published results regarding the effect of cholesterol on %EE of niosomes (Aboelwafa et al, 2010;Thomas & Viswanad, 2012).…”

In-vitro efficacies of topical microemulsions of clotrimazole and ketoconazole; and in-vivo performance of clotrimazole microemulsion

“…Transdermal delivery/ skin permeation of CTZ was enhanced through proniosomal gel formulation. The proneosomal gel also showed higher anticandidial activity and it was presumed that the proneosomal formulation may have enhanced drug penetration through fungal cell wall [16]. Hashem were measured using 90 plus particle size analyzer (Brookhaven Instrument Corporation).…”

Transdermal delivery of oxybutynin chloride proniosomal gels for the treatment of overactive bladder

“…The supernatant layer was used for the determination of free drug by high-performance liquid chromatography (HPLC) (Thomas & Viswanad, 2012).…”