Guangdong Provincial Key Laboratory of Advanced Drug Delivery Systems, Guangdong Pharmaceutical University, Guangzhou, 510000, China.
College of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, 510000, China.
Curr Drug Deliv. 2023;20(10):1525-1532. doi: 10.2174/1567201819666220819110128.
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.
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.
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.
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.
地奈德经皮给药无效，因为其溶解度差。作为一种新的经皮给药系统，纳米乳凝胶在药物传递方面优于传统制剂，具有显著优势。我们已经建立了地奈德纳米乳凝胶（DES NE 凝胶）以实现更好的经皮吸收，但仍需要评估其疗效和安全性。本研究旨在提供额外的证据，证明通过纳米乳凝胶改善地奈德的经皮传递的药效学和安全性。
使用地奈德作为参考制剂，评估地奈德纳米乳凝胶的药效学和安全性。为了评估 DES NE 凝胶与地奈德的疗效差异，并确保安全性，我们使用 2,4-二硝基氟苯（DNFB）建立了 KM 小鼠特应性皮炎（AD）模型。采用耳肿胀度、耳质量差、胸腺、脾脏指数和小鼠 HE 常规病理学作为药效学评价指标，新西兰兔表皮刺激试验预测其刺激性。
纳米乳凝胶可能通过影响皮肤状况促进药物的经皮渗透。中高剂量的 DES NE 凝胶可显著改善皮炎/湿疹引起的小鼠耳部炎症和肿胀。此外，与 DES 凝胶相比，皮肤刺激程度并未增加。
纳米乳凝胶可用于提高低效力或溶解度差的药物的疗效。DES NE 凝胶比其他给药系统具有更高的经皮潜力。在这项研究中，发现纳米乳凝胶是地奈德有前途的经皮载体。DES NE-GEL 对小鼠模型中的皮炎/湿疹具有显著疗效，有望通过经皮系统为皮炎/湿疹的临床治疗提供一种新的、高效、低毒的制剂。
