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.
Int J Mol Sci. 2024 Aug 29;25(17):9389. doi: 10.3390/ijms25179389.
The objective of the study was to develop a novel topical gel by mixing ethanolic extract, thermosensitive poloxamer 407, and carbomer 940 and evaluating its stability and rheological behavior. The irritation potential of the gel was evaluated in accordance with the Organization for Economic Cooperation and Development Guidelines 404. The potential anti-inflammatory effects of the developed gel were evaluated in rats using the carrageenan-induced paw edema test. Moreover, the binding affinity for chlorogenic and ellagic acid, as dominant components in the extract, against cyclooxygenase (COX) 1 and 2 was also determined. Our findings suggest that the gel containing extract remained stable throughout the observation period, exhibited pseudoplastic behavior, and caused no irritation in rats, thus being considered safe for topical treatment. Additionally, the developed gel showed the capability to reduce rat paw edema, which highlights significant anti-inflammatory potential. analysis revealed that chlorogenic and ellagic acid exhibited a reduced binding affinity against COX-1 but had a similar inhibitory effect on COX-2 as flurbiprofen, which was confirmed by molecular dynamics results. The study proposes the possible application of ethanolic extract gel for the alleviation of localized inflammatory diseases; however, future clinical evaluation is required.
本研究的目的是通过混合乙醇提取物、热敏性泊洛沙姆 407 和卡波姆 940 来开发一种新型的局部凝胶,并评估其稳定性和流变学特性。按照经济合作与发展组织准则 404 评估了凝胶的刺激性潜力。采用角叉菜胶诱导的足肿胀试验评估了所开发的凝胶在大鼠体内的潜在抗炎作用。此外,还测定了作为提取物中主要成分的绿原酸和鞣花酸与环氧化酶(COX)1 和 2 的结合亲和力。我们的研究结果表明,含有提取物的凝胶在整个观察期间保持稳定,表现出假塑性行为,且在大鼠体内无刺激性,因此被认为可安全用于局部治疗。此外,所开发的凝胶显示出减轻大鼠足肿胀的能力,这突出了其显著的抗炎潜力。分析表明,绿原酸和鞣花酸对 COX-1 的结合亲和力降低,但对 COX-2 的抑制作用与氟比洛芬相似,这一结果得到了分子动力学结果的证实。本研究提出了将 乙醇提取物凝胶应用于缓解局部炎症性疾病的可能性;然而,需要进行进一步的临床评估。