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通过槲皮素的抗脂质过氧化活性评估其作为原料及在不同局部用制剂中的功能稳定性。

Evaluation of functional stability of quercetin as a raw material and in different topical formulations by its antilipoperoxidative activity.

作者信息

Casagrande Rúbia, Georgetti Sandra R, Verri Waldiceu A, Jabor José R, Santos Antonio C, Fonseca Maria J V

机构信息

Department of Pharmaceutical Science, Faculty of Pharmaceutical Sciences of Ribeirao Preto, University of Sao Paulo, Av do Café s/n, CEP 14040-903, Ribeirão Preto, SP, Brazil.

Department of Food and Drugs Technology, Agricultural Sciences Center, Londrina State University, Paraná, Brazil.

出版信息

AAPS PharmSciTech. 2006 Mar;7(1):E64-E71. doi: 10.1208/pt070110. Epub 2017 Mar 8.

Abstract

The present study evaluates the antioxidant activity of the flavonol quercetin, and its functional stability as a raw material and when added in formulations. The iron-chelating activity was determined using the bathophenanthroline assay, and the functional stability was evaluated with the antilipoperoxidative assay. Raw material presented concentration-dependent antilipoperoxidative and iron-chelating activities. The initial antilipoperoxidative activity of the raw material, cream and gel-cream were 63%, 78%, and 69%, respectively. There was no detectable loss of activity during 182 days (6 months) of storage at all tested temperatures (4°C, room temperature [RT], 37°C, and 45°C) for the raw material. Considering the method variability of 10%, activity loss greater than 10% for nonionic cream was detected after 126 days at 4°C (20.1%), decreasing thereafter to 22.2% after 182 days. At 45°C, the loss of activity started after 182 days (13.2%). For the anionic gel-cream, activity loss started after 84 days (28.4%, 45°C), decreasing after 182 days to 40.3% at 45°C. At 37°C, activity loss was detected after 182 days (12%). In conclusion, the results suggest that the activity of quercetin depends on iron chelation, and its posible usefulness as a topical antioxidant to prevent oxidative stress-induced skin damage depends on maintaining its antilipoperoxidative activity stored at RT, which avoids special storage conditions.

摘要

本研究评估了黄酮醇槲皮素的抗氧化活性,以及其作为原料和添加到配方中时的功能稳定性。使用邻二氮菲测定法测定铁螯合活性,并通过抗脂质过氧化测定法评估功能稳定性。原料呈现出浓度依赖性的抗脂质过氧化和铁螯合活性。原料、乳膏和凝胶乳膏的初始抗脂质过氧化活性分别为63%、78%和69%。在所有测试温度(4°C、室温[RT]、37°C和45°C)下,原料在储存182天(6个月)期间未检测到活性损失。考虑到方法变异性为10%,非离子乳膏在4°C下储存126天后检测到活性损失大于10%(20.1%),此后在182天后降至22.2%。在45°C下,活性损失在182天后开始(13.2%)。对于阴离子凝胶乳膏,活性损失在84天后开始(45°C时为28.4%),在45°C下182天后降至40.3%。在37°C下,182天后检测到活性损失(12%)。总之,结果表明槲皮素的活性取决于铁螯合作用,其作为局部抗氧化剂预防氧化应激诱导的皮肤损伤的潜在用途取决于在室温下储存时保持其抗脂质过氧化活性,这避免了特殊的储存条件。

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