Cutaneous delivery of α-tocopherol and lipoic acid using microemulsions: influence of composition and charge.
Cutaneous delivery of α-tocopherol and lipoic acid using microemulsions: influence of composition and charge.
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DOI：
10.1111/jphp.12045
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发表时间：
2013-06
期刊：
影响因子：
--
通讯作者：
Lopes LB
中科院分区：
文献类型：
--
作者：
Cichewicz A;Pacleb C;Connors A;Hass MA;Lopes LB
评估微乳剂的组成和电荷是否影响其同时将α-生育酚和硫辛酸递送至活性皮肤层的能力。将α-生育酚和硫辛酸（分别为1.1%和0.5% w/w）加入含单-二辛酸甘油酯的癸基葡萄糖苷微乳液中。表征了含有60：30：10（ME-O）和46：23：31（ME-W）的表面活性剂：油：水（w/w/w）的微乳液以及含有1%植物鞘氨醇（ME-Wphy）的阳离子形式的ME-W，并评价了它们破坏皮肤屏障和在皮肤中体外递送抗氧化剂的能力。使用硫代巴比妥酸反应性物质（TBARS）测定评估ME-Wphy处理的皮肤中的抗氧化活性。微乳液的内相直径在47.0-53.2 nm之间;添加植物鞘氨醇并将pH调节至5.0将zeta电位从-4.3 mV增加至+29.1 mV。ME-O呈w/o结构，ME-W和ME-Wphy呈o/w结构。微乳剂影响皮肤电阻和经皮水分损失，但不影响硫辛酸渗透。α-生育酚释放量按ME-O<ME-W<ME-Wphy的顺序增加。ME-Wphy呈现合适的短期稳定性。ME-Wphy提供的抗氧化剂降低了TBARS皮肤水平。尽管微乳液结构仅影响生育酚渗透，但两种抗氧化剂的递送水平足以降低TBARS，支持它们用于增强保护。
To assess whether the composition and charge of microemulsions affect their ability to simultaneously deliver α-tocopherol and lipoic acid into viable skin layers. α-tocopherol and lipoic acid were added (1.1 and 0.5% w/w, respectively) to decylglucoside-based microemulsions containing mono-dicaprylin. Microemulsions containing surfactant:oil:water (w/w/w) at 60:30:10 (ME-O) and 46:23:31 (ME-W), as well as a cationic form of ME-W containing 1% phytosphingosine (ME-Wphy) were characterized, and their ability to disrupt the skin barrier and deliver the antioxidants in vitro in the skin was evaluated. Antioxidant activity in ME-Wphy-treated skin was assessed using the thiobarbituric acid-reactive substances (TBARS) assay. internal phase diameters of microemulsions ranged between 47.0–53.2 nm; phytosphingosine addition and pH adjustment to 5.0 increased zeta potential from −4.3 to +29.1 mV. ME-O displayed w/o structure, whereas ME-W and ME-Wphy were consistent with o/w. Microemulsions affected skin electrical resistance and transepidermal water loss, but did not affect lipoic acid penetration. α-Tocopherol delivery increased following the order ME-O<ME-W<ME-Wphy. ME-Wphy presented suitable short-term stability. The antioxidants delivered by ME-Wphy decreased TBARS cutaneous levels. even though microemulsion structure only affected tocopherol penetration, delivered levels of both antioxidants were sufficient for a decrease in TBARS, supporting their use for enhanced protection.
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