Ethosomes-based topical delivery system of antihistaminic drug for treatment of skin allergies

Abstract

Cetirizine is indicated for the treatment of allergic conditions such as insect bites and stings, atopic and contact dermatitis, eczema, urticaria. This investigation deals with development of a novel ethosome-based topical formulation of cetirizine dihydrochloride for effective delivery. The optimised formulation consisting of drug, phospholipon 90 G™ and ethanol was characterised for drug content, entrapment efficiency, pH, vesicular size, spreadability and rheological behaviour. The ex vivo permeation studies through mice skin showed highest permeation flux (16.300 ± 0.300 µg/h/cm²) and skin retention (20.686 ± 0.517 µg/cm²) for cetirizine-loaded ethosomal vesicles as compared to conventional formulations. The in vivo pharmacodynamic evaluation of optimised formulation was assessed against oxazolone-induced atopic dermatitis (AD) in mice. The parameters evaluated were reduction in scratching score, erythema score, skin hyperplasia and dermal eosinophil count. Our results suggest that ethosomes are effective carriers for dermal delivery of antihistaminic drug, cetirizine, for the treatment of AD.

• Cetirizine
• ethosomes
• hapten
• levocetirizine
• skin allergy

Acknowledgements

The authors gratefully acknowledge gift samples of levocetirizine dihydrochloride and cetirizine dihydrochloride supplied by IndSwift Ltd., India; Phospholipon® 90G, provided by Phospholipid GmbH, Nattermannallee, Koln, Germany; and Carbopol 980 NF from Lubrizol Advanced Materials India Private Limited, Mumbai, India.