Anti-Inflammatory Property Establishment of Fulvic Acid Transdermal Patch in Animal Model

IF 2.3 Q3 PHARMACOLOGY & PHARMACY
Maria A. Konnova, Alexander A. Volkov, Anna G. Solovyeva, Peter V. Peretyagin, Nina B. Melnikova
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Abstract

The formulation of the transdermal patch with fulvic acid (FA) on an emulsion basis using pluronic Kolliphor® p237 as a permeability enhancer was developed and studied for anti-inflammatory properties. FA was isolated from the peat in the Nizhny Novgorod region of Russia and characterized as a potential active pharmaceutical ingredient. In vitro studies of the release of FA from the transdermal patch, as well as the FA penetration through the acetyl cellulose membrane using the Franz diffusion cell, showed its high efficiency (56% and 90%, respectively, in 8 h). In the in vivo experiment, qualitative and quantitative features of the rat knee caused by complete Freund’s adjuvant-induced arthritis (morphological changes, the FA influence on the biochemical indexes) were studied. The inflammatory process that developed within 15 days was accompanied by the activation of antioxidant oxidoreductase enzymes (by 50–70%), the increase in the cross-sectional diameter of the cartilage, and the increase in the values of marker indicators of the process of rheumatoid arthritis. Within 7 days of treatment, under the influence of FA, the values of ESR, RF, leukocytes, C-reactive protein, as well as the biochemical parameters characterizing oxidative stress (SOD, catalase, glutathione reductase, LDH, G6PD) normalized, and the edema reduced. These results may be useful for arthritis treatment using the transdermal patch with FA.
黄腐酸透皮贴剂抗炎作用的动物模型建立
采用pluronic Kolliphor®p237作为渗透性增强剂,开发了黄腐酸(FA)乳液型透皮贴剂配方,并研究了其抗炎性能。FA是从俄罗斯下诺夫哥罗德地区的泥炭中分离出来的,被认为是一种潜在的活性药物成分。体外研究了FA在透皮贴片中的释放,以及Franz扩散池对乙酰纤维素膜的渗透,在8 h内分别达到56%和90%。在体内实验中,研究了完全Freund佐剂诱导的大鼠膝关节的定性和定量特征(形态学改变,FA对生化指标的影响)。15天内发展的炎症过程伴随着抗氧化还原酶的激活(50-70%),软骨横截面直径的增加,类风湿关节炎过程的标志物指标值的增加。治疗7天内,在FA的影响下,ESR、RF、白细胞、c反应蛋白及表征氧化应激的生化指标(SOD、过氧化氢酶、谷胱甘肽还原酶、LDH、G6PD)恢复正常,水肿减轻。这些结果可能对使用FA透皮贴片治疗关节炎有用。
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来源期刊
Scientia Pharmaceutica
Scientia Pharmaceutica Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
4.60
自引率
4.00%
发文量
67
审稿时长
10 weeks
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