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 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.
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Interpretation of studies claiming benefit from antioxidant supplements or topical creams for photoaging is confounded by complex formulation of interventions, with most studies using a cocktail of compounds and topical creams providing a moisturising effect.
“Although there are a number of studies that claim a significant benefit from an antioxidant supplement or topical cream, interpretation of the data is confounded by the complex formulation of the interventions, with most studies using a cocktail of compounds and with the formulation of topical creams providing a moisturising effect in itself [23,61,88,154].”
From The Roles of Vitamin C in Skin Health. (2017) · cites this paper as [61]
A special formulation that involves removing the ionic charge from L-ascorbic acid is needed to enhance penetration.
“Special formulation that involves removing of the ionic charge from the molecule is needed to enhance penetration (89).”
From Photoprotection: a Review of the Current and Future Technologies (2010) · cites this paper as [89]
Vitamins C and E interact synergistically to protect each other and increase overall effectiveness.
“Vitamins C and E interact synergistically to protect each other and increase overall effectiveness (Pinnell et al, 2001).”
From Ferulic Acid Stabilizes a Solution of Vitamins C and E and Doubles its Photoprotection of Skin (2005) · cites this paper as Pinnell et al, 2001
Fifteen percent L-ascorbic acid saturates skin in 3 d; its tissue half-life is about 4 d.
“Fifteen percent L-ascorbic acid saturates skin in 3 d; its tissue half life is about 4 d (Pinnell et al, 2001).”
From Ferulic Acid Stabilizes a Solution of Vitamins C and E and Doubles its Photoprotection of Skin (2005) · cites this paper as Pinnell et al, 2001
The solution must be formulated at pH 3.5 or lower for vitamin C to be absorbed into skin.
“The solution must be formulated at a pH of 3.5 or lower for the vitamin C to be absorbed into skin: at this pH the vitamin C is protonated and the molecule is uncharged (Pinnell et al, 2001).”
From Ferulic Acid Stabilizes a Solution of Vitamins C and E and Doubles its Photoprotection of Skin (2005) · cites this paper as Pinnell et al, 2001
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“Although there are a number of studies that claim a significant benefit from an antioxidant supplement or topical cream, interpretation of the data is confounded by the complex formulation of the interventions, with most studies using a cocktail of compounds and with the formulation of topical creams providing a moist…”
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- Authors
- Pinnell, S. R., Yang, H., Omar, M., Riviere, N. M., DeBuys, H. V., Walker, L. C., Wang, Y., & Levine, M.
- Affiliations
- Duke Medical Center (US)
- North Carolina State University (US)
- National Institutes of Health (US)
- Corresponding author
- Pinnell, Sheldon R.
- ORCID
- Wang, Yaohui
- Venue
- Dermatologic Surgery
- Published
- 2001-02
- Volume
- 27
- Issue
- 2
- Pages
- 137-142
- ISSN
- 1076-0512 (ISSN-L)
- 1524-4725
- OpenAlex
- W2171899001
- Cited by
- 213
- References
- 5
- Citations by year
- 2026: 5 · 2025: 13 · 2024: 14 · 2023: 18 · 2022: 17 · 2021: 15 · 2020: 15 · 2019: 10 · 2018: 8 · 2017: 7 · 2016: 11 · 2015: 7 · 2014: 5 · 2013: 3 · 2012: 7
- FWCI
- 5.61
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Dermatologic Surgery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Dermatology › Skin Protection and Aging
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › melanin and skin pigmentation
- Keywords
- vitamin C, topical vitamin C, percutaneous absorption, skin penetration, antioxidants, photoaging, photocarcinogenesis, magnesium ascorbyl phosphate, dehydroascorbic acid, porcine skin, tissue concentration
- MeSH terms
- Administration, Cutaneous, Animals, Antioxidants, Ascorbic Acid, Dehydroascorbic Acid, Hydrogen-Ion Concentration, Skin, Skin Absorption, Sunscreening Agents, Swine
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