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基于癸基葡萄糖苷的微乳液用于番茄红素和抗坏血酸的经皮定位。

Decylglucoside-based microemulsions for cutaneous localization of lycopene and ascorbic acid.

机构信息

Albany College of Pharmacy and Health Sciences, Albany, NY 12208, USA.

出版信息

Int J Pharm. 2012 Sep 15;434(1-2):420-8. doi: 10.1016/j.ijpharm.2012.06.016. Epub 2012 Jun 9.

Abstract

Cutaneous delivery of combinations of antioxidants offers the possibility of enhanced protection against UV-radiation. In this study, we investigated the potential of sugar-based microemulsions containing monoglycerides to promote simultaneous cutaneous delivery of lycopene and ascorbic acid, and increase tissue antioxidant activity. Lycopene and ascorbic acid were incorporated (0.04% and 0.2% (w/w), respectively) in decylglucoside-based microemulsions containing isopropyl myristate mixed with monocaprylin (ME-MC), monolaurin (ME-ML) or monoolein (ME-MO) as oil phase. The microemulsions increased lycopene delivery into porcine ear skin by 3.3- to 8-fold compared to a drug solution. The effect of microemulsions on ascorbic acid cutaneous delivery was more modest (1.5-3-fold), and associated with an approximately 2-fold increase in transdermal delivery. According to their penetration-enhancing ability, the microemulsions were ranked ME-MC>ME-MO>ME-ML. This superiority of ME-MC coincided with a stronger effect in decreasing skin electrical resistance. After 18 h of treatment, the viability of bioengineered skin treated with ME-MC was 2.2-times higher compared to Triton-X100 (moderate irritant), demonstrating that ME-MC is less cytotoxic. Skin treatment with ME-MC containing both antioxidants increased the tissue antioxidant activity by 10.2-fold, but no synergism between the antioxidants was observed.

摘要

基于糖的微乳含有单甘酯,具有促进番茄红素和抗坏血酸同时经皮传递的潜力,并能增加组织抗氧化活性。将番茄红素和抗坏血酸(分别为 0.04%和 0.2%(w/w))掺入含有肉豆蔻酸异丙酯与辛酸/癸酸甘油三酯(ME-MC)、月桂酸单甘油酯(ME-ML)或油酸单甘油酯(ME-MO)的丙二醇基微乳中。与药物溶液相比,微乳使番茄红素进入猪耳朵皮肤的传递增加了 3.3-8 倍。微乳对抗坏血酸经皮传递的影响更为温和(1.5-3 倍),并使透皮传递增加了约 2 倍。根据其增强渗透能力,微乳的排名为 ME-MC>ME-MO>ME-ML。ME-MC 的这种优势与降低皮肤电阻的更强作用一致。经过 18 小时的处理,用 ME-MC 处理的生物工程皮肤的存活率比 Triton-X100(中度刺激性)高 2.2 倍,表明 ME-MC 的细胞毒性更小。用含有两种抗氧化剂的 ME-MC 处理皮肤可使组织抗氧化活性增加 10.2 倍,但抗氧化剂之间没有协同作用。

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