Cited by 97Skin Protection and AgingAdvancements in Transdermal Drug DeliveryCollagen: Extraction and Characterization

Vitamin C–squalene bioconjugate promotes epidermal thickening and collagen production in human skin

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Gref, R., Deloménie, C., Maksimenko, A., Gouadon, E., Percoco, G., Lati, E., Desmaële, D., Zouhiri, F. +1 more·2020·Scientific Reports

Abstract

Vitamin C (Vit C) benefits to human skin physiology notably by stimulating the biosynthesis of collagen. The main cutaneous collagens are types I and III, which are less synthesized with aging. Vit C is one of the main promotors of collagen formation but it poorly bypasses the epidermis stratum corneum barrier. To address this challenge, we developed a lipophilic version of Vit C for improving skin diffusion and delivery. Vit C was covalently conjugated to squalene (SQ), a natural lipid of the skin, forming a novel Vit C–SQ derivative suitable for cream formulation. Its biological activity was investigated on human whole skin explants in an ex vivo model, through histology and protein and gene expression analyses. Results were compared to Vit C coupled to the reference lipophilic compound palmitic acid, (Vit C–Palmitate). It was observed that Vit C–SQ significantly increased epidermal thickness and preferentially favored collagen III production in human skin after application for 10 days. It also promoted glycosaminoglycans production in a higher extent comparatively to Vit C–Palmitate and free Vit C. Microdissection of the explants to separate dermis and epidermis allowed to measure higher transcriptional effects either in epidermis or in dermis. Among the formulations studied, the strongest effects were observed with Vit C–SQ.

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  1. [10]Nielsen, M. J. & Karsdal M. A. Biochemistry of collagens, laminins and elastin. structure, function and biomarkers (ed. Karsdal, M. A.) 21–30 (Elsevier, 2016).

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Authors
Gref, R., Deloménie, C., Maksimenko, A., Gouadon, E., Percoco, G., Lati, E., Desmaële, D., Zouhiri, F., & Couvreur, P.
Affiliations
  • Centre National de la Recherche Scientifique (FR)
  • Université Paris-Saclay (FR)
  • Hypertension pulmonaire : physiopathologie et innovation thérapeutique (FR)
Corresponding author
  • Gref, R.
  • Couvreur, P.
Venue
Scientific Reports
Published
2020-10-09
Volume
10
Issue
1
Pages
16883-16883
ISSN
2045-2322 (ISSN-L)
OpenAlex
W3091899464
Cited by
97
References
54
Citations by year
2026: 8 · 2025: 19 · 2024: 20 · 2023: 30 · 2022: 15 · 2021: 4 · 2020: 1
FWCI
9.09
Type
journal article
Language
en
Open access
Locations
  • Scientific Reports (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • HAL (submittedVersion)
  • HAL (submittedVersion, other-oa)
  • HAL (submittedVersion, cc-by)
Funders
  • Agence Nationale de la Recherche (ANR-10-LABX-0035)
  • European Research Council (249835249835)
Topics
  • Health Sciences › Medicine › Dermatology › Skin Protection and Aging
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
  • Physical Sciences › Materials Science › Biomaterials › Collagen: Extraction and Characterization
Keywords
vitamin C, squalene, bioconjugates, type III collagen, epidermal thickening, stratum corneum barrier, glycosaminoglycans, skin explants, topical cream formulation, palmitic acid, skin aging
MeSH terms
Adult, Ascorbic Acid, Collagen, Drug Compounding, Epidermis, Female, Humans, Skin, Squalene, Drug Delivery Systems, In Vitro Techniques

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