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使用化学和草药增强剂增加阿达帕林的递送。

Increase adapalene delivery using chemical and herbal enhancers.

机构信息

Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

Department of Pharmaceutics, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.

出版信息

J Cosmet Dermatol. 2021 Sep;20(9):3011-3017. doi: 10.1111/jocd.13960. Epub 2021 Feb 2.

Abstract

BACKGROUND

Acne is one of the skin diseases that include abnormalities in the production of sebum, changes in the microbial flora, abnormal keratinization, and inflammation. Adapalene is a good choice in the treatment of acne with fewer side effects and high effectiveness. However, the absorption of adapalene through human skin is low. We investigated the effect of several enhancers on the skin absorption of adapalene.

METHODS

For the preparation of a topical formulation, this drug needs proper skin absorption. Therefore, to increase the effect of chemical absorption of the Adapalene skin permeability, it should first be put on the skin in a touch of some absorption like Eucalyptus, Urea, Clove oil, propylene glycol, and oleic acid for 1 and 2 hours and was then examined for the passing of the drug on the treated skin and for the effect of absorptions by calculating of the permeability parameters using DSC and FT-IR techniques.

RESULT AND CONCLUSION

The results show that the enhancers used increased the permeability of the drug adapalene to water. Several mechanisms including lipid liquefaction, degradation of the fat structure, as well as irreversible denaturation of intracellular creatine caused by Eucalyptus, urea clove oil, PG, and oleic acid are the main mechanisms of drug penetration. Based on the results, it was found that among the enhancers studied, eucalyptus and urea had the highest and the lowest absorption effect in 2- and 1-hour pre-contact, respectively.

摘要

背景

痤疮是一种皮肤病,包括皮脂产生异常、微生物菌群变化、异常角质化和炎症等。阿达帕林是治疗痤疮的较好选择,副作用少,疗效高。然而,阿达帕林通过人体皮肤的吸收率较低。我们研究了几种促进剂对阿达帕林皮肤吸收的影响。

方法

为了制备局部制剂,该药物需要适当的皮肤吸收。因此,为了提高阿达帕林皮肤化学吸收的效果,首先应该在皮肤上涂抹一些吸收剂,如桉树油、尿素、丁香油、丙二醇和油酸 1 到 2 小时,然后检查药物在处理过的皮肤上的穿透情况,并通过 DSC 和 FT-IR 技术计算渗透率参数来评估吸收效果。

结果与结论

结果表明,所使用的促进剂增加了阿达帕林向水中的渗透性。桉树油、尿素、丁香油、PG 和油酸等促进剂的主要渗透机制包括脂质液化、脂肪结构降解以及细胞内肌酸的不可逆变性。基于这些结果,发现在所研究的促进剂中,桉树油和尿素在 2 小时和 1 小时预接触时的吸收效果最高和最低。

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