Efficient Topical Delivery of Chlorogenic Acid by an Oil-in-Water Microemulsion to Protect Skin against UV-Induced Damage
Efficient Topical Delivery of Chlorogenic Acid by an Oil-in-Water Microemulsion to Protect Skin against UV-Induced Damage
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DOI：
10.1248/cpb.59.793
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发表时间：
2011-06-01
影响因子：
1.7
通讯作者：
Teraoka, Reiko
中科院分区：
文献类型：
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作者：
Kitagawa, Shuji;Yoshii, Kenta;Teraoka, Reiko
我们通过体外研究，使用切除的豚鼠背部皮肤和尤卡坦微型猪皮肤，检查了亲水多酚绿原酸的皮内递送。绿原酸在皮肤中的蓄积和溶解度比槲皮素和染料木素等其他多酚大得多。然而，由于增强皮肤输送似乎是必要的，以显示其对皮肤氧化损伤的保护作用，我们研究了微乳液作为载体的作用。用150 MM NaCl溶液、肉豆酸异丙酯、山梨糖聚氧乙烯单油酸酯（吐温80）和乙醇组成的微乳液，绿原酸的皮肤蓄积量和溶解度进一步增加。水包油（o/w型）微乳的增强效果大于油包水（w/o型）微乳，这可能是由于溶解度的增加更大。这一发现与之前对槲皮素和染料木素等相对疏水性多酚的研究结果大不相同。用含绿原酸的微乳凝胶预处理豚鼠背部皮肤，可预防紫外线照射引起的红斑。这些发现表明亲水绿原酸与o/w型微乳液作为一种载体可以保护皮肤免受紫外线引起的氧化损伤。
We examined the intradermal delivery of a hydrophilic polyphenol chlorogenic acid by in vitro study using excised guinea pig dorsal skin and Yucatan micropig skin. Skin accumulation as well as the solubility of chlorogenic acid in aqueous vehicles was much greater than for other polyphenols such as quercetin and genistein. However, since enhancement of skin delivery seemed to be necessary to exhibit its protective effects against oxidative damage of skin, we examined the effects of microemulsions as vehicles. Using microemulsions consisting of 150 MM NaCl solution, isopropyl myristate, polyoxyethylene sorbitan monooleate (Tween 80) and ethanol, skin accumulation as well as solubility of chlorogenic acid further increased. Enhancement effect of an oil-in-water (o/w-type) microemulsion was greater than that of a water-in-oil (w/o-type) microemulsion possibly due to the greater increase in solubility. This finding was quite different from previous findings on relatively hydrophobic polyphenols such as quercetin and genistein. Pretreatment of guinea pig dorsal skin with chlorogenic acid containing microemulsion gel prevented erythema formation induced by UV irradiation. These findings indicate the potential use of hydrophilic chlorogenic acid with o/w-type microemulsion as a vehicle to protect skin against UV-induced oxidative damage.