Itraconazole loaded ethosomal gel system for efficient treatment of skin cancer

Manish Kumar Gupta, Swarnlata Saraf

Abstract


Topical application of Itraconazole for the treatment of Basal cell carcinoma represents a new hope in dermatology. Itraconazole for treatment of Basal cell carcinoma is an alternative therapeutic approach for the efficacious treatment of nonmelanoma skin cancer. Itraconazole loaded ethosomes were prepared and characterized by vesicular shape, vesicular size, entrapment efficiency. Ethosomal gel were prepared and characterized by pH, viscosity, washability, spreadibility, drug content, drug release study, stability study, in vivo skin tolerability and antiproliferative activity. Transmission Electron Microscopy (TEM), and Dynamic Light Scattering (DLS) characterise ethosomes as spherical, unilamellar structures having low polydispersity (0.384 ± 0.037) and nanometric size range (169.0 ± 49.0), % Entrapment efficiency of Itraconazole in ethosomal carrier was found to be 82.00 ± 1.78. Ethosomal gel were prepared by using Carbopol. The viscosity was found to be in the range of 1600±1.72 to 1740±1.73 cps. The spreadability was found to be in the range of 6.4g.cm/sec. The drug content of the ethosomal gel formulations ranged from 0.384-0.386 mg/gm. The value of steady-state transdermal flux was observed to be 54.2 ± 1.46 µg/h/cm with a lag time of 1.2 hrs with formulation EG1. Stability studies revealed no noticeable changes in drug release profile occurred. Skin irritation study on rabbit skin suggested that ethosomal gel may offer a suitable approach for transdermal delivery of Itraconazole. The further, antiproliferative study shows that Itraconazole loaded ethosomes is significantly more toxic than the free drug on BCC1/KMC cell line, thus making it a potential alternative to the standard therapy.


Keywords


Ethosomal gel, Itraconazole, Basal cell carcinoma, Antiproliferative study, skin irritation study.

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