Cited by 346Skin Protection and AgingPhytochemicals and Antioxidant ActivitiesAdvancements in Transdermal Drug Delivery

In vitro and in vivo evaluation of caffeic and ferulic acids as topical photoprotective agents

Saija, A·2000·International Journal of Pharmaceutics

Abstract

Topically-applied antioxidant drugs represent a successful strategy for protecting the skin against UV-mediated oxidative damage. However, they can afford to the skin a satisfactory photoprotection only if able to permeate through the stratum corneum and thus to reach deeper cutaneous layers. Caffeic and ferulic acids, dissolved in saturated aqueous solutions at pH 3 or 7.2, have been tested for their capability to permeate through excised human skin mounted in Franz cells. At both pH values, ferulic and, at a lower degree, caffeic acids appeared able to permeate through the stratum corneum. The known higher lipophilicity of ferulic acid may explain the fact that it permeates through the stratum corneum better than caffeic acid. However, vehicle pH values proved to have no influence on biophenol skin permeation profile; this observed lack of pH effect may reflect the drug higher concentration attainable in saturated solutions at high pH. On the basis of the findings obtained in these in vitro experiments, we designed the schedule of a series of in vivo experiments, carried out to evaluate the ability of caffeic and ferulic acids to reduce, in healthy human volunteers, UVB-induced skin erythema, monitored by means of reflectance spectrophotometry. Caffeic and ferulic acids, dissolved in saturated aqueous solution pH 7.2, proved to afford a significant protection to the skin against UVB-induced erythema. To conclude, we have confirmed, by means of in vitro and in vivo experimen…

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Crossref · 10.1016/s0378-5173(00)00358-6

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Authors
Saija, A.
Affiliations
Sapienza University of Rome (IT)
Corresponding author
Saija, A
Venue
International Journal of Pharmaceutics
Publisher
Elsevier BV
Published
2000-04-10
Volume
199
Issue
1
Pages
39-47
ISSN
0378-5173 (ISSN-L)
OpenAlex
W2023313329
Cited by
346
References
2
Citations by year
2026: 13 · 2025: 11 · 2024: 15 · 2023: 12 · 2022: 15 · 2021: 19 · 2020: 22 · 2019: 14 · 2018: 15 · 2017: 16 · 2016: 17 · 2015: 21 · 2014: 14 · 2013: 15 · 2012: 13
FWCI
6.37
Type
journal article
Language
en
Open access
closed
Locations
  • International Journal of Pharmaceutics (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Dermatology › Skin Protection and Aging
  • Health Sciences › Medicine › Biochemistry › Phytochemicals and Antioxidant Activities
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
Keywords
caffeic acid, ferulic acid, photoprotection, topical antioxidants, skin permeation, stratum corneum, Franz diffusion cell, saturated aqueous solutions, percutaneous absorption
MeSH terms
Administration, Topical, Adult, Caffeic Acids, Chromatography, High Pressure Liquid, Coumaric Acids, Erythema, Female, Humans, Hydrogen-Ion Concentration, Skin Absorption, Spectrophotometry, Ultraviolet, Sunscreening Agents, Ultraviolet Rays, Area Under Curve, In Vitro Techniques

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