Topical L-ascorbic Acid: Percutaneous Absorption Studies

Dermatol Surg. 2001 Feb;27(2):137-42. doi: 10.1046/j.1524-4725.2001.00264.x.

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 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.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Antioxidants / administration & dosage*
  • Antioxidants / pharmacokinetics*
  • Ascorbic Acid / administration & dosage*
  • Ascorbic Acid / analogs & derivatives
  • Ascorbic Acid / pharmacokinetics*
  • Dehydroascorbic Acid / administration & dosage
  • Dehydroascorbic Acid / pharmacokinetics
  • Hydrogen-Ion Concentration
  • Skin / metabolism
  • Skin Absorption*
  • Sunscreening Agents / administration & dosage*
  • Sunscreening Agents / pharmacokinetics*
  • Swine

Substances

  • Antioxidants
  • Sunscreening Agents
  • Ascorbic Acid
  • Dehydroascorbic Acid