地奈德纳米乳凝胶经皮吸收给药:药效学和安全性评价。

IF 2.8 4区医学 Q2 PHARMACOLOGY & PHARMACY Current drug delivery Pub Date : 2023-01-01 DOI:10.2174/1567201819666220819110128

Jiaqi Zhang, Yu Yao, Hanbing Liu, Qiuyan Ma, Lanyi Huang, Yuan Chen, Huaqing Lin

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引用次数: 1

摘要

背景:经皮给药时，地奈德由于溶解度差而无效。纳米乳凝胶作为一种新型的透皮给药系统，在给药方面具有传统给药方式无法比拟的优势。我们已经建立了地奈德纳米乳凝胶(DES NE凝胶)，具有更好的透皮吸收效果，但其有效性和安全性仍有待评价。本研究旨在提供额外的证据，证明通过纳米乳凝胶经皮给药地奈德的药效学和安全性得到改善。方法:以地奈德®为参比制剂，评价地奈德纳米乳凝胶的药效学和安全性。为了评估DES - NE凝胶与地索酸钠(Desonate®)的疗效差异，并确保安全性，采用2,4-二硝基氟苯(DNFB)建立KM小鼠特应性皮炎(AD)模型。以小鼠耳肿胀程度、耳肿块差、胸腺、脾脏指数、HE常规病理作为药效学评价指标，采用新西兰兔表皮刺激法预测刺激效果。结果:纳米乳凝胶可通过影响皮肤状况促进药物的透皮渗透。中、高剂量DES NE凝胶可显著改善小鼠皮炎/湿疹引起的耳部炎症和肿胀。此外，与DES凝胶相比，皮肤刺激程度没有增加。结论:纳米乳凝胶可用于提高低效或溶解度差的药物的疗效。DES - NE凝胶提供了比其他输送系统更高的透皮潜能。本研究发现纳米乳凝胶是一种很有前景的经皮DES载体，DES NE-GEL在小鼠皮炎/湿疹模型中具有显著的疗效，有望为临床经皮治疗皮炎/湿疹提供一种新型、高效、低毒的制剂。

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Desonide Nanoemulsion Gel for Transdermal Absorption Drug Delivery: Pharmacodynamic and Safety Evaluation.

Background: When administered transdermally, desonide is ineffective due to its poor solubility. As a new transdermal delivery system, nanoemulsion gel has demonstrated significant advantages for drug delivery over conventional formulations. We have established desonide nanoemulsion gel (DES NE gel) for better transdermal absorption, but its efficacy and safety still need to be evaluated. This study aims to provide additional evidence demonstrating the improved pharmacodynamics and safety of transdermal delivery of Desonide via nanoemulsion gel.

Methods: Pharmacodynamics and safety of Desonide nanoemulsion gel were evaluated using Desonate ^® as the reference formulation. To assess the difference in curative effect between DES NE gel and Desonate^® and to ensure safety, atopic dermatitis (AD) models in KM mice were developed using 2,4-dinitrofluorobenzene (DNFB). The degree of ear swelling, ear mass difference, thymus, spleen index, and HE conventional pathology of mice were used as pharmacodynamic evaluation indexes, and the irritation was predicted by the New Zealand rabbit epidermal stimulation assay.

Results: Nanoemulsion gels may facilitate transdermal penetration of drugs by influencing the skin condition. Medium and high doses of DES NE gel significantly ameliorated the inflammation and swelling of the ear caused by dermatitis/eczema in mice. In addition, compared with DES gel, skin irritation extent did not increase.

Conclusion: Nanoemulsion gel can be applied to improve the efficacy of drugs with low potency or poor solubility. DES NE gel provides a higher transdermal potential than other delivery systems. In this study, it was found that nanoemulsion gel is a promising percutaneous carrier of DES. DES NE-GEL has a significant curative effect on dermatitis/eczema in a mouse model and is expected to provide a new, efficient, and low toxic preparation for clinical treatment of dermatitis/eczema through the percutaneous system.

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来源期刊

Current drug delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.10

自引率

4.20%

发文量

170

期刊介绍： Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.