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天然油脂酶促衍生黄酮酯的皮肤渗透:凝胶乳液的释放机制、稳定性及皮肤相容性

skin permeation of flavonoid esters enzymatically derived from natural oils: release mechanism from gel emulsion, stability, and dermatological compatibility.

作者信息

Milivojević Ana, Ćorović Marija, Petrov Ivanković Anja, Simović Milica, Banjanac Katarina, Pjanović Rada, Bezbradica Dejan

机构信息

Faculty of Technology and Metallurgy, Department of Biochemical Engineering and Biotechnology, University of Belgrade, Belgrade, Serbia.

Innovation Center of Faculty of Technology and Metallurgy, Belgrade, Serbia.

出版信息

Pharm Dev Technol. 2024 Dec;29(10):1121-1132. doi: 10.1080/10837450.2024.2424977. Epub 2024 Nov 9.

DOI:10.1080/10837450.2024.2424977
PMID:39498532
Abstract

Due to their broad spectrum of biological activities and attractive pharmacological properties, flavonoids are very promising molecules for application in skin care products. In this study, phloridzin and naringin medium- and long-chain fatty acid esters were enzymatically synthesized in reaction with natural oils (coconut and linseed oil) and transdermal delivery of synthesized esters through artificial Strat-M membrane was investigated. Experimental results were succesfully fitted using Peppas and Sahlin model which includes the phase. Release kinetics of all examined flavonoid esters from gel emulsions through the membrane depended on both diffusion and polymer relaxation effect (0.5< < 1). The estimated effective diffusion coefficients ranged from 0.168·10 to 6.149·10 cm s for phloridzin esters and from 0.116·10 to 4.210·10 cm s for naringin esters. The effective diffusion coefficients decreased with the increase in ester molecular weight indicating the size-dependent diffusion. All formulation showed good stability, excellent hydration effect, and excellent dermatological compatibility without irritating effect. It can be concluded that gel emulsions with a mixture of flavonoid esters enzymatically synthesized in reaction with vegetable oils can be effectively topically applied as a skin care products.

摘要

由于黄酮类化合物具有广泛的生物活性和诱人的药理特性,它们是应用于护肤品的非常有前景的分子。在本研究中,根皮苷和柚皮苷的中长链脂肪酸酯通过与天然油(椰子油和亚麻籽油)反应进行酶法合成,并研究了合成酯通过人工Strat-M膜的透皮递送。实验结果成功地用包括相的Peppas和Sahlin模型进行了拟合。所有检测的黄酮类酯从凝胶乳液通过膜的释放动力学取决于扩散和聚合物松弛效应(0.5< <1)。根皮苷酯的估计有效扩散系数范围为0.168·10至6.149·10 cm²/s,柚皮苷酯的估计有效扩散系数范围为0.116·10至4.210·10 cm²/s。有效扩散系数随着酯分子量的增加而降低,表明扩散与尺寸有关。所有配方均显示出良好的稳定性、出色的保湿效果和出色的皮肤相容性,且无刺激作用。可以得出结论,与植物油反应酶法合成的黄酮类酯混合物的凝胶乳液可有效地作为护肤品局部应用。

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