Background

Topical drug delivery offers improved therapeutic effect and reduced systemic adverse effects of the administered compounds.

Objective

The present work was aimed at developing and comparing levocetirizine loaded polymeric nanoparticles and niosomal formulation(s), respectively, against dinitrochlorobenzene-induced atopic dermatitis animal model.

Methods

The niosome and chitosan nanoparticle were developed and evaluated for particle size distribution, drug loading, and entrapment efficiency. The formulations were optimized through Box-Behnken design. The optimized formulations were dispersed in carbopol gel and evaluated for ex vivo permeation, retention, and in vivo studies.

Results

The optimized niosomes and chitosan nanoparticle exhibited a particle size range of 384.4 ± 64.3 nm and 382.7 ± 59.2 nm, drug loading of 18.99 ± 0.02% and 12.2 ± 1.6%, and entrapment efficiency of 46.63 ± 2.12% and 29.6 ± 1.6%, respectively. The permeation and retention studies displayed less permeation and significantly (p < 0.01) high retention percentage of LCZD by OPT-N gel when compared with OPT-CN gel. In in vivo studies revealed that OPT-N significantly (p < 0.05) reduces erythema score (from 3 to 1) and scratching frequency (70–25 scratches/20 min).

Conclusion

OPT-N gel shows high entrapment efficiency and skin retention capacity of the drug along with better topical applicability and higher therapeutic efficacy. The OPT-N also manifested the maximum peripheral action of LCZD against AD as compared with optimized chitosan gel and plain LCZD gel.

中文翻译：

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左西替利嗪负载的囊泡和基质类型系统局部应用的比较研究：对特应性皮炎的治疗潜力评估

背景

局部药物递送提供了改善的治疗效果并降低了所施用化合物的全身性不良反应。

目的

本工作旨在针对二硝基氯苯诱导的特应性皮炎动物模型分别开发和比较负载左西替利嗪的聚合物纳米颗粒和脂质体制剂。

方法

开发了纳米脂质体和壳聚糖纳米颗粒，并对其粒径分布，载药量和包封效率进行了评估。通过Box-Behnken设计优化了配方。将优化的制剂分散在卡波姆凝胶中，并进行离体渗透，保留和体内研究。

结果

优化的脂质体和壳聚糖纳米颗粒的粒径范围为384.4±64.3 nm和382.7±59.2 nm，载药量分别为18.99±0.02％和12.2±1.6％，包封率分别为46.63±2.12％和29.6±1.6％ 。 与OPT-CN凝胶相比，OPT-N凝胶对LCZD的渗透和保留研究显示较少的渗透和显着（p <0.01）高LCZD保留百分比。体内研究表明，OPT-N显着降低（p  <0.05）红斑评分（从3降低到1）和刮擦频率（70–25刮擦/ 20分钟）。

结论

OPT-N凝胶显示出药物的高包封效率和皮肤保留能力，以及更好的局部适用性和更高的治疗功效。与优化的壳聚糖凝胶和普通LCZD凝胶相比，OPT-N还表现出LCZD对AD的最大外周作用。