Aim: This work aimed to develop topical nanoemulsion gels of cetirizine, a second-generation antihistamine, to avoid its oral intake drawbacks and enhance skin permeation.

Methods: Cetirizine nanoemulsions were formulated and characterised for their particle size, polydispersity index, zeta potential, drug release and drug permeation through rat skin. The optimised formulation, obtained using 2³ full factorial design, was incorporated in carbopol and chitosan gels and evaluated clinically for urticaria treatment.

Results: The optimised formulation had particle size of 32.015 ± 1.87 nm, polydispersity index of 0.29 ± 0.04, zeta potential of –19.31 ± 0.43 mV, cetirizine percent released of 98.50 ± 1.23% and permeability coefficient of 7.65 cm.h⁻¹. Cetirizine nanoemulsion gels were more effective than their control gels in urticaria treatment with significant decrease in the degree of wheals and itching and higher recovery percent.

Conclusion: Cetirizine nanoemulsion topical gels are expected to be a rational and effective tool for avoiding cetirizine oral side effects and targeting the affected skin.

目的：这项工作旨在开发第二代抗组胺药西替利嗪的局部纳米乳胶，以避免其口服摄入不足并增强皮肤渗透性。

方法：制备西替利嗪纳米乳剂，并对其粒径，多分散指数，ζ电势，药物释放和药物在大鼠皮肤中的渗透进行表征。使用2 ³全因子设计获得的优化配方被掺入卡波普凝胶和壳聚糖凝胶中，并进行临床评估以用于荨麻疹治疗。

结果：优化后的配方粒径为32.015±1.87 nm，多分散指数为0.29±0.04，ζ电位为–19.31±0.43 mV，西替利嗪释放百分数为98.50±1.23％，渗透系数为7.65 cm.h ^-1。西替利嗪纳米乳胶在荨麻疹治疗中比其对照凝胶更有效，风团和瘙痒程度明显降低，回收率更高。

结论：西替利嗪纳米乳局部用凝胶有望成为避免西替利嗪口服副作用并靶向受影响皮肤的合理有效工具。