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载壬二酸固体脂质纳米分散体水凝胶经皮给药系统增强药物渗透、疗效和安全性评价,以克服特应性皮炎治疗障碍。

Drug permeation enhancement, efficacy, and safety assessment of azelaic acid loaded SNEDDS hydrogel to overcome the treatment barriers of atopic dermatitis.

机构信息

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, 110062, India.

School of Pharmacy, Monash University, Bandar Sunway, Jalan Lagoon Selatan, 47500, Malaysia.

出版信息

Environ Res. 2023 Nov 1;236(Pt 2):116850. doi: 10.1016/j.envres.2023.116850. Epub 2023 Aug 7.


DOI:10.1016/j.envres.2023.116850
PMID:37558118
Abstract

Atopic dermatitis is one of the most widespread chronic inflammatory skin conditions that can occur at any age, though the prevalence is highest in children. The purpose of the current study was to prepare and optimize the azelaic acid (AzA) loaded SNEDDS using Pseudo ternary phase diagram, which was subsequently incorporated into the Carbopol 940 hydrogel for the treatment of atopic dermatitis. The composition was evaluated for size, entrapment efficiency, in vitro, ex vivo, and in vivo studies. The polydispersity index of the optimized preparation was found to be less than 0.5, and the size of the distributed globules was found to be 151.20 ± 3.67 nm. The SNEDDS hydrogel was characterized for pH, viscosity, spreadability, and texture analysis. When compared to the marketed formulation, SNEDDS hydrogel was found to have a higher rate of permeation through the rat skin. In addition, a skin irritation test carried out on experimental animals showed that the SNEDDS formulation did not exhibit any erythematous symptoms after a 24-h exposure. In conclusion, the topical delivery of AzA through the skin using SNEDDS hydrogel could prove to be an effective approach for the treatment of atopic dermatitis.

摘要

特应性皮炎是一种最广泛的慢性炎症性皮肤疾病,可以在任何年龄发生,尽管在儿童中患病率最高。本研究的目的是使用伪三元相图来制备和优化载有壬二酸(AzA)的 SNEDDS,随后将其纳入 Carbopol 940 水凝胶中用于治疗特应性皮炎。对组合物进行了评价,包括粒径、包封效率、体外、离体和体内研究。优化制剂的多分散指数发现小于 0.5,且分布液滴的粒径为 151.20±3.67nm。对 SNEDDS 水凝胶进行了 pH 值、粘度、铺展性和质地分析。与市售制剂相比,SNEDDS 水凝胶被发现具有更高的通过大鼠皮肤的渗透速率。此外,在实验动物上进行的皮肤刺激性试验表明,SNEDDS 制剂在 24 小时暴露后没有出现任何红斑症状。总之,通过 SNEDDS 水凝胶经皮给予 AzA 可能是治疗特应性皮炎的一种有效方法。

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Drug permeation enhancement, efficacy, and safety assessment of azelaic acid loaded SNEDDS hydrogel to overcome the treatment barriers of atopic dermatitis.

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[2]
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[4]
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[5]
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