Topical L-ascorbic acid: Percutaneous absorption studies

Abstract

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 pigskin. 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.

Sheldon R. Pinnell, MD ; Huanshu Yang, MD ; Mostafa Omar, PhD ; Nancy Monteiro Riviere, PhD ; Holly V. DeBuys, MD ; Linda C. Walker ; Yaohui Wang, MD ; and Mark Levine, MD