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同时对硫辛酸和白藜芦醇进行纳米包封以改善皮肤的抗氧化性能。

Simultaneous nanoencapsulation of lipoic acid and resveratrol with improved antioxidant properties for the skin.

作者信息

Davies Samuel, Contri Renata Vidor, Guterres Silvia Stanisçuaski, Pohlmann Adriana Raffin, Guerreiro Irene Clemes Kulkamp

机构信息

Programa de Pós Graduação em Ciências farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Brazil.

Programa de Pós Graduação em Ciências farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Brazil; Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Brazil.

出版信息

Colloids Surf B Biointerfaces. 2020 Aug;192:111023. doi: 10.1016/j.colsurfb.2020.111023. Epub 2020 Apr 12.

Abstract

Cutaneous aging is intimately related to redox imbalance, which is mainly caused by ultraviolet radiation exposure. The aim of the present investigation was to develop lipid-core nanocapsules for the co-nanoencapsulation of resveratrol and lipoic acid aiming to improve the chemical stability and photostability of the compounds, as well as their antioxidant properties. Lipid-core nanocapsules were developed and characterized according to their mean size, size distribution, zeta potential, pH value, drug content, encapsulation efficiency, release profile, stability under storage, photostability and skin permeation profile. In vitro antioxidant activity was analyzed by lipid peroxidation method and the in vitro cytotoxicity by MTT assay and cellular count, using BALB/c-3T3 fibroblasts. It was possible to co-nanoencapsulate resveratrol and lipoic acid into particles of average diameter close to 200 nm, low polydispersity index and encapsulation efficiencies around 90 %. Nanoencapsulation increased the substances stability under storage and photostability under UVA light exposure, besides controlling substances release. The actives were able to permeate a skin model membrane when nanoencapsulated, with a faster permeation of lipoic acid. The antioxidant activity was potentiated by the co-nanoencapsulation of resveratrol and lipoic acid, without signs of cytotoxicity to fibroblasts. Therefore, the co-nanoencapsulation of resveratrol and lipoic acid is promising for application in topical formulations aiming antioxidant effects.

摘要

皮肤老化与氧化还原失衡密切相关,氧化还原失衡主要由紫外线照射引起。本研究的目的是开发脂质核纳米胶囊,用于共纳米包封白藜芦醇和硫辛酸,旨在提高化合物的化学稳定性和光稳定性以及它们的抗氧化性能。根据脂质核纳米胶囊的平均尺寸、尺寸分布、zeta电位、pH值、药物含量、包封效率、释放曲线、储存稳定性、光稳定性和皮肤渗透曲线对其进行了开发和表征。采用脂质过氧化法分析体外抗氧化活性,采用MTT法和细胞计数法分析体外细胞毒性,使用BALB/c-3T3成纤维细胞。可以将白藜芦醇和硫辛酸共纳米包封到平均直径接近200nm、多分散指数低且包封效率约为90%的颗粒中。纳米包封除了控制物质释放外,还提高了物质在储存时的稳定性和在紫外线A照射下的光稳定性。当纳米包封时,活性成分能够渗透皮肤模型膜,硫辛酸的渗透更快。白藜芦醇和硫辛酸的共纳米包封增强了抗氧化活性,对成纤维细胞没有细胞毒性迹象。因此,白藜芦醇和硫辛酸的共纳米包封有望应用于具有抗氧化作用的局部制剂中。

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