Vitamin C–squalene bioconjugate promotes epidermal thickening and collagen production in human skin
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 corn...
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| Veröffentlicht in: | Scientific reports 2020-10, Vol.10 (1), p.16883-16883, Article 16883 |
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| creator | Gref, R. Deloménie, C. Maksimenko, A. Gouadon, E. Percoco, G. Lati, E. Desmaële, D. Zouhiri, F. Couvreur, P. |
| description | 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. |
| doi_str_mv | 10.1038/s41598-020-72704-1 |
| format | Article |
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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.</description><identifier>ISSN: 2045-2322</identifier><identifier>EISSN: 2045-2322</identifier><identifier>DOI: 10.1038/s41598-020-72704-1</identifier><identifier>PMID: 33037252</identifier><language>eng</language><publisher>London: Nature Publishing Group UK</publisher><subject>631/92/152 ; 631/92/2783 ; Adult ; Ascorbic Acid - metabolism ; Ascorbic Acid - pharmacology ; Chemical Sciences ; Collagen - biosynthesis ; Drug Compounding ; Drug Delivery Systems ; Epidermis - drug effects ; Epidermis - metabolism ; Female ; Galenic pharmacology ; Humanities and Social Sciences ; Humans ; In Vitro Techniques ; Life Sciences ; multidisciplinary ; Pharmaceutical sciences ; Science ; Science (multidisciplinary) ; Skin - drug effects ; Skin - metabolism ; Squalene</subject><ispartof>Scientific reports, 2020-10, Vol.10 (1), p.16883-16883, Article 16883</ispartof><rights>The Author(s) 2020</rights><rights>Distributed under a Creative Commons Attribution 4.0 International License</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c480t-af299d62fd2322c2e138da29948e9b8f0d67e6f018e17e720efbdac6372304a43</citedby><cites>FETCH-LOGICAL-c480t-af299d62fd2322c2e138da29948e9b8f0d67e6f018e17e720efbdac6372304a43</cites><orcidid>0000-0001-7961-5443 ; 0000-0002-6326-966X</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7547010/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7547010/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,727,780,784,864,885,27924,27925,41120,42189,51576,53791,53793</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33037252$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://cnrs.hal.science/hal-03095927$$DView record in HAL$$Hfree_for_read</backlink></links><search><creatorcontrib>Gref, R.</creatorcontrib><creatorcontrib>Deloménie, C.</creatorcontrib><creatorcontrib>Maksimenko, A.</creatorcontrib><creatorcontrib>Gouadon, E.</creatorcontrib><creatorcontrib>Percoco, G.</creatorcontrib><creatorcontrib>Lati, E.</creatorcontrib><creatorcontrib>Desmaële, D.</creatorcontrib><creatorcontrib>Zouhiri, F.</creatorcontrib><creatorcontrib>Couvreur, P.</creatorcontrib><title>Vitamin C–squalene bioconjugate promotes epidermal thickening and collagen production in human skin</title><title>Scientific reports</title><addtitle>Sci Rep</addtitle><addtitle>Sci Rep</addtitle><description>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.</description><subject>631/92/152</subject><subject>631/92/2783</subject><subject>Adult</subject><subject>Ascorbic Acid - metabolism</subject><subject>Ascorbic Acid - pharmacology</subject><subject>Chemical Sciences</subject><subject>Collagen - biosynthesis</subject><subject>Drug Compounding</subject><subject>Drug Delivery Systems</subject><subject>Epidermis - drug effects</subject><subject>Epidermis - metabolism</subject><subject>Female</subject><subject>Galenic pharmacology</subject><subject>Humanities and Social Sciences</subject><subject>Humans</subject><subject>In Vitro Techniques</subject><subject>Life Sciences</subject><subject>multidisciplinary</subject><subject>Pharmaceutical sciences</subject><subject>Science</subject><subject>Science (multidisciplinary)</subject><subject>Skin - drug effects</subject><subject>Skin - metabolism</subject><subject>Squalene</subject><issn>2045-2322</issn><issn>2045-2322</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><sourceid>C6C</sourceid><sourceid>EIF</sourceid><recordid>eNp9kc9u1DAQxi1ERattX4AD8hEOAf_LOr4gVSugSCtxoVwtrz3JepvYWzupxI134A15EhxSqsKhvtia-eY3nvkQeknJW0p48y4LWqumIoxUkkkiKvoMnTEi6opxxp4_ep-ii5wPpJyaKUHVC3TKOeGS1ewMwTc_msEHvPn142e-nUwPAfDORxvDYerMCPiY4hBHyBiO3kEaTI_Hvbc3EHzosAkO29j3poMwS91kRx8DLsj9NJiA840P5-ikNX2Gi_t7ha4_fvi6uaq2Xz593lxuKysaMlamZUq5NWvd_G_LgPLGmRITDahd0xK3lrBuCW2ASpCMQLtzxq7LLJwII_gKvV-4x2k3gLMQxmR6fUx-MOm7jsbrfzPB73UX77SshSRlryv0ZgHs_yu7utzqOUY4UbVi8o4W7ev7ZineTpBHPfhsoawiQJyyZkIoVUsh6iJli9SmmHOC9oFNiZ7t1Iudutip_9ipZ_6rx8M8lPw1rwj4IsglFTpI-hCnFMqCn8L-Bq8FrZk</recordid><startdate>20201009</startdate><enddate>20201009</enddate><creator>Gref, R.</creator><creator>Deloménie, C.</creator><creator>Maksimenko, A.</creator><creator>Gouadon, E.</creator><creator>Percoco, G.</creator><creator>Lati, E.</creator><creator>Desmaële, D.</creator><creator>Zouhiri, F.</creator><creator>Couvreur, P.</creator><general>Nature Publishing Group UK</general><general>Nature Publishing Group</general><scope>C6C</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>1XC</scope><scope>VOOES</scope><scope>5PM</scope><orcidid>https://orcid.org/0000-0001-7961-5443</orcidid><orcidid>https://orcid.org/0000-0002-6326-966X</orcidid></search><sort><creationdate>20201009</creationdate><title>Vitamin C–squalene bioconjugate promotes epidermal thickening and collagen production in human skin</title><author>Gref, R. ; Deloménie, C. ; Maksimenko, A. ; Gouadon, E. ; Percoco, G. ; Lati, E. ; Desmaële, D. ; Zouhiri, F. ; Couvreur, P.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c480t-af299d62fd2322c2e138da29948e9b8f0d67e6f018e17e720efbdac6372304a43</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>631/92/152</topic><topic>631/92/2783</topic><topic>Adult</topic><topic>Ascorbic Acid - metabolism</topic><topic>Ascorbic Acid - pharmacology</topic><topic>Chemical Sciences</topic><topic>Collagen - biosynthesis</topic><topic>Drug Compounding</topic><topic>Drug Delivery Systems</topic><topic>Epidermis - drug effects</topic><topic>Epidermis - metabolism</topic><topic>Female</topic><topic>Galenic pharmacology</topic><topic>Humanities and Social Sciences</topic><topic>Humans</topic><topic>In Vitro Techniques</topic><topic>Life Sciences</topic><topic>multidisciplinary</topic><topic>Pharmaceutical sciences</topic><topic>Science</topic><topic>Science (multidisciplinary)</topic><topic>Skin - drug effects</topic><topic>Skin - metabolism</topic><topic>Squalene</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Gref, R.</creatorcontrib><creatorcontrib>Deloménie, C.</creatorcontrib><creatorcontrib>Maksimenko, A.</creatorcontrib><creatorcontrib>Gouadon, E.</creatorcontrib><creatorcontrib>Percoco, G.</creatorcontrib><creatorcontrib>Lati, E.</creatorcontrib><creatorcontrib>Desmaële, D.</creatorcontrib><creatorcontrib>Zouhiri, F.</creatorcontrib><creatorcontrib>Couvreur, P.</creatorcontrib><collection>Springer Nature OA Free Journals</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Hyper Article en Ligne (HAL)</collection><collection>Hyper Article en Ligne (HAL) (Open Access)</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Scientific reports</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Gref, R.</au><au>Deloménie, C.</au><au>Maksimenko, A.</au><au>Gouadon, E.</au><au>Percoco, G.</au><au>Lati, E.</au><au>Desmaële, D.</au><au>Zouhiri, F.</au><au>Couvreur, P.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Vitamin C–squalene bioconjugate promotes epidermal thickening and collagen production in human skin</atitle><jtitle>Scientific reports</jtitle><stitle>Sci Rep</stitle><addtitle>Sci Rep</addtitle><date>2020-10-09</date><risdate>2020</risdate><volume>10</volume><issue>1</issue><spage>16883</spage><epage>16883</epage><pages>16883-16883</pages><artnum>16883</artnum><issn>2045-2322</issn><eissn>2045-2322</eissn><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.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>33037252</pmid><doi>10.1038/s41598-020-72704-1</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0001-7961-5443</orcidid><orcidid>https://orcid.org/0000-0002-6326-966X</orcidid><oa>free_for_read</oa></addata></record> |
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| subjects | 631/92/152 631/92/2783 Adult Ascorbic Acid - metabolism Ascorbic Acid - pharmacology Chemical Sciences Collagen - biosynthesis Drug Compounding Drug Delivery Systems Epidermis - drug effects Epidermis - metabolism Female Galenic pharmacology Humanities and Social Sciences Humans In Vitro Techniques Life Sciences multidisciplinary Pharmaceutical sciences Science Science (multidisciplinary) Skin - drug effects Skin - metabolism Squalene |
| title | Vitamin C–squalene bioconjugate promotes epidermal thickening and collagen production in human skin |
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