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

Current drug delivery(2023)

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摘要
Backgrounds: When administered transdermally, desonide has an unsatisfactory effectiveness 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 that 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 the safety, the 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 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 the higher transdermal potential than other delivery systems. In this study, it was found that nano-emulsion gel is a promising percutaneous carrier of DES. DES NE-GEL has significant curative effect on dermatitis/eczema in mouse model, and is expected to provide a new, efficient and low toxic preparation for clinical treatment of dermatitis/eczema through percutaneous system.
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关键词
Desonide,nanoemulsion gel,pharmacodynamic research,safety evaluation,eczema,potency
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