外用L-抗坏血酸：经皮吸收研究。
Topical L-ascorbic acid: percutaneous absorption studies.
作者信息
Pinnell S R, Yang H, Omar M, Monteiro-Riviere N, DeBuys H V, Walker L C, Wang Y, Levine M
机构信息
Duke University Medical Center, Department of Medicine, Durham, North Carolina 27707, USA.
出版信息
Dermatol Surg. 2001 Feb;27(2):137-42. doi: 10.1046/j.1524-4725.2001.00264.x.
BACKGROUND
Reactive oxygen species generated by ultraviolet light result in photocarcinogenic and photoaging changes in the skin. Antioxidants protect skin from these insults.
OBJECTIVE
This study defines formulation characteristics for delivering L-ascorbic acid into the skin to supplement the skin's natural antioxidant reservoir.
METHODS
L-ascorbic acid or its derivatives were applied to pig skin. Skin levels of L-ascorbic acid were measured to determine percutaneous delivery.
RESULTS
L-ascorbic acid must be formulated at pH levels less than 3.5 to enter the skin. Maximal concentration for optimal percutaneous absorption was 20%. Tissue levels were saturated after three daily applications; the half-life of tissue disappearance was about 4 days. Derivatives of ascorbic acid including magnesium ascorbyl phosphate, ascorbyl-6-palmitate, and dehydroascorbic acid did not increase skin levels of L-ascorbic acid.
CONCLUSIONS
Delivery of topical L-ascorbic acid into the skin is critically dependent on formulation characteristics.
背景
紫外线产生的活性氧会导致皮肤发生光致癌和光老化变化。抗氧化剂可保护皮肤免受这些损伤。
目的
本研究确定将L-抗坏血酸输送到皮肤中以补充皮肤天然抗氧化剂储备的配方特性。
方法
将L-抗坏血酸或其衍生物应用于猪皮。测量皮肤中L-抗坏血酸的水平以确定经皮递送情况。
结果
L-抗坏血酸必须在pH值低于3.5的条件下配制才能进入皮肤。最佳经皮吸收的最大浓度为20%。每日应用三次后组织水平达到饱和；组织消失的半衰期约为4天。抗坏血酸的衍生物，包括磷酸镁抗坏血酸酯、抗坏血酸-6-棕榈酸酯和脱氢抗坏血酸，并未提高皮肤中L-抗坏血酸的水平。
结论
局部L-抗坏血酸向皮肤中的递送严重依赖于配方特性。
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