In vitro evaluation of quercetin cutaneous absorption from topical formulations and its functional stability by antioxidant activity
In vitro evaluation of quercetin cutaneous absorption from topical formulations and its functional stability by antioxidant activity
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DOI：
10.1016/j.ijpharm.2006.08.006
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发表时间：
2007-01-10
影响因子：
5.8
通讯作者：
Fonseca, Maria J. V.
中科院分区：
文献类型：
--
作者：
Casagrande, Rubia;Georgetti, Sandra R.;Fonseca, Maria J. V.
最近，有研究证明两种不同的含有槲皮素的制剂可以抑制UVB诱导的皮肤氧化应激和炎症反应。因此，在本研究中，采用改良的Franz扩散池，通过抗氧化活性、制剂中槲皮素的释放以及其皮肤保留性来评价这些制剂的功能稳定性。两种配方(1)高脂肪含量的非离子乳剂和(2)低脂肪含量的阴离子乳剂)在180d内保持功能(供氢能力)稳定。此外，根据硝酸纤维素膜的测定，两种制剂中都释放了槲皮素。通过抑制丙二醛的形成，观察了两种制剂中保留在皮肤中的槲皮素的体外抗氧化活性。在配方1中，槲皮素保留率的影响是时间依赖的。结论是，这项研究表明，在配方1中，槲皮素在功能上保持稳定，并且测量抗氧化活性是在组织产品干扰最小的情况下评估槲皮素皮肤保留率的有效方法。此外，目前关于皮肤保留的结果解释了先前关于槲皮素在体内的活性的研究，这些数据表明，含有槲皮素的制剂可能被用作局部活性产品来控制UVB介导的皮肤氧化损伤。(C)2006爱思唯尔B.V.保留所有权利。
Recently, it was demonstrated that two different formulations containing quercetin inhibit the UVB-induced cutaneous oxidative stress and inflammation. Therefore, in the present study it was evaluated the functional stability of those formulations by the antioxidant activity, the release of quercetin from the formulations, and its skin retention using modified Franz diffusion cells. Both formulations tested ((1) non-ionic emulsion with high lipid content and (2) anionic emulsion with low lipid content) remained functionally (hydrogen-donating ability) stable during 180 days. Furthermore, quercetin was released from both formulations as determined using nitrocellulose membrane. In vitro antioxidant activity of retained quercetin into the skin was observed for both formulations as detected by the inhibition of malondialdehyde formation. The effect of quercetin retention was time-dependent for formulation 1. Concluding, this study demonstrates that quercetin remains functionally stable in formulations, and measuring the antioxidant activity is an efficient approach to evaluate quercetin skin retention with minimal interference of the tissue products. Furthermore, the present results on skin retention explain the previous study on quercetin in vivo activities, and together, these data suggest that formulations containing quercetin may be used as topical active products to control UVB-mediated oxidative damage of the skin. (c) 2006 Elsevier B.V. All rights reserved.