<p>The present research aims to explore the ex vivo permeability and toxicity of ciclopirox olamine (CO)–loaded transferosomal topical gel using goat ear pinna via Franz diffusion cells and HaCaT cell lines, respectively. The transferosomes were formulated by the Rotary evaporation-sonication process. The composition of transferosomes includes lipids, viz., soya lecithin, and cholesterol at a 5:1 ratio; edge activators, i.e., Tween 80, and sodium deoxycholate at a 1:3 ratio; and lipid dissolving solvent system, i.e., chloroform, and ethanol at 3:1 ratio, along with 0.77% w/w of CO. The developed transferosomes exhibited a vesicle size of 121.4 ± 76.4&#xa0;nm, polydispersity index 0.336, a negative zeta potential value of − 15.1 ± 5.74&#xa0;mV, and 99.35 ± 0.34% entrapment efficiency. The developed transferosome dispersion was further loaded in Carbopol 940 gels at three varying concentrations, viz. 0.5%w/v, 1%w/v, and 1.5%w/v. Furthermore, each transferosomal gel was characterized for visual inspection, pH, and rheological characteristics. Based on viscosity, out of three gel formulations, the selected gel with 6.88 ± 1.02 pH and viscosity of 25,700 ± 412 cps was subjected to further studies, viz. texture analysis, drug content, anti-fungal studies, ex vivo permeation analysis, toxicity against HaCaT cell lines, and stability studies as per ICH guidelines.</p> Graphical Abstract <p></p>

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In Vitro Toxicity, Safety, and Skin Permeability Evaluation of Antifungal Transferosomal Hydrogels for the Advanced Management of Foot Dermatophytosis

  • Triveni Tiwari,
  • Shreya Kaul,
  • Upendra Nagaich,
  • Manisha Pandey,
  • Dinesh Kumar Mishra,
  • Neha Jain

摘要

The present research aims to explore the ex vivo permeability and toxicity of ciclopirox olamine (CO)–loaded transferosomal topical gel using goat ear pinna via Franz diffusion cells and HaCaT cell lines, respectively. The transferosomes were formulated by the Rotary evaporation-sonication process. The composition of transferosomes includes lipids, viz., soya lecithin, and cholesterol at a 5:1 ratio; edge activators, i.e., Tween 80, and sodium deoxycholate at a 1:3 ratio; and lipid dissolving solvent system, i.e., chloroform, and ethanol at 3:1 ratio, along with 0.77% w/w of CO. The developed transferosomes exhibited a vesicle size of 121.4 ± 76.4 nm, polydispersity index 0.336, a negative zeta potential value of − 15.1 ± 5.74 mV, and 99.35 ± 0.34% entrapment efficiency. The developed transferosome dispersion was further loaded in Carbopol 940 gels at three varying concentrations, viz. 0.5%w/v, 1%w/v, and 1.5%w/v. Furthermore, each transferosomal gel was characterized for visual inspection, pH, and rheological characteristics. Based on viscosity, out of three gel formulations, the selected gel with 6.88 ± 1.02 pH and viscosity of 25,700 ± 412 cps was subjected to further studies, viz. texture analysis, drug content, anti-fungal studies, ex vivo permeation analysis, toxicity against HaCaT cell lines, and stability studies as per ICH guidelines.

Graphical Abstract