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新开发的含提取物半固体制剂:表征、稳定性评估、安全性及抗炎活性研究

Newly Developed Semi-Solid Formulations Containing Extract: Characterization, Assessment of Stability, Safety, and Anti-Inflammatory Activity.

作者信息

Bradic Jovana, Petrovic Anica, Nikolic Milos, Nedeljkovic Nikola, Andjic Marijana, Kladar Nebojsa, Bolevich Stefani, Jakovljevic Vladimir, Kocovic Aleksandar

机构信息

Department of Pharmacy, Faculty of Medical Sciences, University of Kragujevac, 34000 Kragujevac, Serbia.

Center of Excellence for Redox Balance Research in Cardiovascular and Metabolic Disorders, 34000 Kragujevac, Serbia.

出版信息

Pharmaceutics. 2024 Jul 29;16(8):1003. doi: 10.3390/pharmaceutics16081003.

Abstract

has been traditionally used as an anti-inflammatory agent; nevertheless, a comprehensive evaluation of its efficacy and safety and comparison with standard drugs are lacking. Taking into consideration concerns with current therapies, like efficacy limitations, side effects, and resistance, we aimed to develop a natural gel and cream based on extract and explore their anti-inflammatory potential. After the chemical analysis of the extract confirmed the presence of coumarin, -coumaric acid, gallic acid, and quercetin, formulations were prepared and subjected to physical and chemical stability evaluations over 6 months. The safety potential was tested in rats, while the anti-inflammatory activity was assessed both via in silico tests and in a rat model of inflammation. The examined formulations showed stable physical characteristics at the defined storage conditions and did not exert any sign of adverse skin reaction. The gel formulation exhibited a remarkable effect in inflammation reduction comparable with hydrocortisone. The in silico results suggest that coumarin, -coumaric, and gallic acid bind to COX-1 and COX-2 with a lower affinity compared to diclofenac. On the other hand, quercetin demonstrated comparable inhibitory activity and stronger interaction compared to the control drug. Our results indicate that the examined formulations are stable and safe and may be promising dermal products for the alleviation of inflammatory skin conditions.

摘要

传统上它被用作抗炎剂;然而,缺乏对其疗效和安全性的全面评估以及与标准药物的比较。考虑到当前疗法存在的问题,如疗效局限性、副作用和耐药性,我们旨在开发一种基于提取物的天然凝胶和乳膏,并探索它们的抗炎潜力。在对提取物进行化学分析确认存在香豆素、对香豆酸、没食子酸和槲皮素后,制备了制剂并在6个月内进行了物理和化学稳定性评估。在大鼠身上测试了其安全潜力,同时通过计算机模拟测试和大鼠炎症模型评估了其抗炎活性。所检测的制剂在规定的储存条件下显示出稳定的物理特性,并且没有出现任何皮肤不良反应的迹象。凝胶制剂在减轻炎症方面表现出与氢化可的松相当的显著效果。计算机模拟结果表明,与双氯芬酸相比,香豆素、对香豆酸和没食子酸与COX-1和COX-2的结合亲和力较低。另一方面,与对照药物相比,槲皮素表现出相当的抑制活性和更强的相互作用。我们的结果表明,所检测的制剂稳定且安全,可能是用于缓解炎症性皮肤病的有前景的皮肤产品。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0c0d/11359922/9784a3c184f5/pharmaceutics-16-01003-g001.jpg

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