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基于没食子酸和羟基酪醇的抗氧化表面活性剂的皮肤递送

Skin delivery of antioxidant surfactants based on gallic acid and hydroxytyrosol.

作者信息

Alonso Cristina, Lucas Ricardo, Barba Clara, Marti Meritxell, Rubio Laia, Comelles Francesc, Morales Juan Carlos, Coderch Luisa, Parra José Luís

机构信息

Department of Chemical and Surfactants Technology, Advanced Chemical Institute of Catalonia IQAC-CSIC, Barcelona, Spain.

Chemical Research Institute CSIC, Universidad de Sevilla, Sevilla, Spain.

出版信息

J Pharm Pharmacol. 2015 Jul;67(7):900-8. doi: 10.1111/jphp.12382. Epub 2015 Feb 3.

Abstract

OBJECTIVES

The aim of this study has been to investigate the dermal absorption profile of the antioxidant compounds gallic acid and hydroxytyrosol as well as their derivatives, hexanoate (hexyl gallate and hydroxytyrosol hexanoate) and octanoate (octyl gallate and octanoate derivative) alkyl esters (antioxidant surfactants). Previously, the scavenging capacity of these compounds, expressed as efficient dose ED50, has also determined.

METHODS

The percutaneous absorption of these compounds was obtained by an in vitro methodology using porcine skin biopsies on Franz static diffusion cells. The antiradical activity of compounds was determined using the 1,1-diphenyl-2-picrylhydrazyl free radical method.

KEY FINDINGS

The percutaneous penetration results show the presence of antioxidants in all layers of the skin. The content of the cutaneously absorbed compound is higher for the antioxidant surfactants (ester derivatives). This particular behaviour could be due to the higher hydrophobicity of these compounds and the presence of surface activity in the antioxidant surfactants.

CONCLUSIONS

These new antioxidant surfactants display optimum properties, which may be useful in the preparation of emulsified systems in cosmetic and pharmaceutical formulations because of their suitable surface activity and because they can protect the skin from oxidative damage.

摘要

目的

本研究旨在探究抗氧化化合物没食子酸和羟基酪醇及其衍生物己酸酯(没食子酸己酯和羟基酪醇己酸酯)和辛酸酯(没食子酸辛酯和辛酸酯衍生物)烷基酯(抗氧化表面活性剂)的皮肤吸收情况。此前,还测定了这些化合物以有效剂量ED50表示的清除能力。

方法

采用体外方法,使用猪皮肤活检组织在Franz静态扩散池上获取这些化合物的经皮吸收情况。使用1,1-二苯基-2-苦基肼自由基法测定化合物的抗自由基活性。

主要发现

经皮渗透结果表明皮肤各层均存在抗氧化剂。抗氧化表面活性剂(酯衍生物)的皮肤吸收化合物含量更高。这种特殊行为可能是由于这些化合物具有更高的疏水性以及抗氧化表面活性剂中存在表面活性。

结论

这些新型抗氧化表面活性剂具有最佳性能,因其具有合适的表面活性且能保护皮肤免受氧化损伤,在化妆品和药物制剂的乳化体系制备中可能有用。

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