Full factorial design-based development and characterization of ciclopirox olamine loaded transferosomes: An efficient approach for the management of Athlete's foot

Abstract

The aim of the current research is to develop ciclopirox olamine (CO) loaded transferosomes to achieve enhanced permeation via thickened, dry, scaly, and cracked stratum corneum during athlete's foot, which conventional topical formulation fails to achieve. In addition, the potential of developed formulation was compared with marketed formulation via in vitro antifungal studies. CO-transferosomes were optimized and developed using design of experiment approach viz. 24 full-factorial design and employing four independent variables viz. ratio of edge activators viz. sodium deoxycholate (SDC) and tween 80, ratio of lipids viz. soya lecithin (SL), and cholesterol, ratio of solvent system i.e., chloroform and ethanol and volume of hydrating solvent viz. phosphate buffer saline PBS (pH 7.4). Rotary evaporation-sonication technique was used to formulate transferosomes. Particle size, polydispersity index (PDI), and zeta potential were three selected dependent variables. To comprehend the intricate interaction between the underlying variables and the outcome variables of the developed formulation, the response surface methodology suggested by Design Expert® was found to be desirable with a desirability value of 0.676. Based on desirability function, the optimized formulation was developed and characterized. The results of optimized formulation for particle size were found to be 124.2 ± 5.1 nm, PDI was 0.280 and a negative zeta potential value of −12.20 ± 6.49 mV. Furthermore, the drug entrapment efficiency was found to be 96.56 ± 0.08 % with a release of 95.67 ± 1.05 % at the end of 24h. The results of release kinetics displayed that the release followed Higuchi diffusion kinetics with highest regression coefficient, followed by zero order. Additionally, the formulation was evaluated for in vitro antifungal activity against Trichophyton mentagrophytes which revealed a wider zone of inhibition of 28.05 mm ± 0.86 as compared to the marketed formulation. The results of ex vivo skin permeation studies of CO-loaded transferosomes revealed high permeability of transferosomes with enhancement ratio of 2.2. Based on the promising results, it may be possible to treat athlete's foot with improved cutaneous distribution of ciclopirox olamine using transferosomes.