Cetirizine from topical phosphatidylcholine liposomes: Evaluation of peripheral antihistaminic activity and systemic absorption in a rabbit model

✍ Scribed by Abeer A.W. Elzainy; Xiaochen Gu; F. Estelle R. Simons; Keith J. Simons

• Publisher: John Wiley and Sons
• Year: 2004
• Tongue: English
• Weight: 97 KB
• Volume: 25
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.419

✦ Synopsis

Abstract

This study was performed to assess the peripheral H~1~‐antihistaminic activity and extent of systemic absorption of cetirizine from liposomes applied to the skin. Cetirizine was incorporated into small unilamellar vesicles (SUV) and multilamellar vesicles (MLV) prepared using L‐α‐phosphatidylcholine, and into Glaxal Base (GB), used as the control. In a randomized, cross‐over study, each formulation, containing 10 mg of cetirizine, was applied to depilated areas on the backs of six rabbits (3.08±0.05 kg). Histamine‐induced wheal tests and blood sampling were performed before cetirizine application and at designated times for up to 24 h. Compared with the baseline, histamine‐induced wheal formation was suppressed by cetirizine in SUV and MLV from 0.5–24 h and by cetirizine in GB from 0.5–8 h, p⩽0.05. Maximum wheal suppression by cetirizine in SUV and MLV ranged from 90.6%±4.9% to 89.0%±3.8% and 98.0%±1.3% to 94.0%±2.3%, respectively, from 6 to 8 h. The plasma cetirizine AUC of 201±24.2 ng.h/ml from SUV was lower than from PC‐MLV, 334.6±65.1 ng.h/ml and from GB, 248.3±34.6 ng.h/ml. After 24 h, the percent of the cetirizine dose remaining on the backs of the rabbits from SUV was lower than from both MLV and GB, p⩽0.05. In this model, cetirizine from both SUV and MLV had excellent topical H~1~‐antihistaminic effects, while systemic exposure to cetirizine from SUV was reduced. Copyright © 2004 John Wiley & Sons, Ltd.