Topical L‐Ascorbic Acid: Percutaneous Absorption Studies

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.