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反式白藜芦醇增强的抗氧化作用:与聚乙二醇和环糊精二元体系的潜力

Enhanced antioxidant effect of trans-resveratrol: potential of binary systems with polyethylene glycol and cyclodextrin.

作者信息

Moyano-Mendez Josè Ramon, Fabbrocini Gabriella, De Stefano Daniela, Mazzella Caterina, Mayol Laura, Scognamiglio Immacolata, Carnuccio Rosa, Ayala Fabio, La Rotonda Maria Immacolata, De Rosa Giuseppe

机构信息

Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Seville , Seville , Spain .

出版信息

Drug Dev Ind Pharm. 2014 Oct;40(10):1300-7. doi: 10.3109/03639045.2013.817416. Epub 2013 Jul 17.

Abstract

Trans-resveratrol, a polyphenol extracted from Vitis vinifera, has different beneficial effects following its administration on the skin. Here the potential use of binary systems to enhance in vitro and in vivo activity of trans-resveratrol was investigated. Thus the aqueous solubility of trans-resveratrol was investigated in the presence of growing concentrations of polyethylene glycol (PEG) or β-cyclodextrin (βCD) as solubilizing excipients. Then, the solid dispersion of trans-resveratrol with PEG or inclusion complexes trans-resveratrol/βCD were prepared and characterised by different methods. Cytotoxicity and inhibition of reactive oxygen species (ROS) following H2O2 challenge in the presence of trans-resveratrol, alone or associated to the excipients, was evaluated on human keratinocyte HaCaT cell line. Both the trans-resveratrol-containing binary systems induced significant reduction of H2O2-induced ROS production, especially in the case of βCD that was selected for the following phase of the study. Thus, the effect of a cream containing trans-resveratrol, alone or associated to βCD, on different skin parameters such as corneometry, colorimetry and elastometry, was evaluated on human volunteers. All patients showed a visible improvement of clinical conditions with a remarkable decrease of aging signs, but this effect was higher of the hemi face treated with the βCD-containing formulation versus formulation containing trans-resveratrol alone.

摘要

反式白藜芦醇是一种从葡萄中提取的多酚,其对皮肤具有不同的有益作用。本文研究了二元体系对增强反式白藜芦醇体外和体内活性的潜在用途。因此,研究了在作为增溶辅料的聚乙二醇(PEG)或β-环糊精(βCD)浓度不断增加的情况下反式白藜芦醇的水溶性。然后,制备了反式白藜芦醇与PEG的固体分散体或反式白藜芦醇/βCD包合物,并采用不同方法进行了表征。在人角质形成细胞HaCaT细胞系中,评估了单独或与辅料联合使用的反式白藜芦醇在H2O2刺激后的细胞毒性和对活性氧(ROS)的抑制作用。含反式白藜芦醇的二元体系均能显著降低H2O2诱导的ROS生成,尤其是在被选入后续研究阶段的βCD的情况下。因此,在人类志愿者身上评估了含反式白藜芦醇单独或与βCD联合使用的乳膏对不同皮肤参数(如角质层含水量测定、比色法和弹性测定)的影响。所有患者的临床状况均有明显改善,衰老迹象显著减少,但含βCD制剂治疗的半侧面部的效果优于单独含反式白藜芦醇的制剂。

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