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In vitro skin penetration of acetyl hexapeptide-8 from a cosmetic formulation.
Cutan Ocul Toxicol. 2015 Mar; 34(1):46-52.CO

Abstract

There is a concern that peptides in cosmetic creams marketed as anti-aging/anti-wrinkle may penetrate into the deep layers of the skin and potentially stimulate biological activity. Claims for one cosmetic peptide, acetyl hexapeptide-8 (Ac-EEMQRR-amide), suggest interference with neuromuscular signaling as its anti-wrinkle mechanism of action. Therefore, the skin penetration of commercially available Ac-EEMQRR-amide from a cosmetic formulation (oil-in-water (O/W) emulsion) was determined in hairless guinea pig (HGP) and human cadaver skin assembled into in vitro diffusion cells. An O/W emulsion containing 10% Ac-EEMQRR-amide was applied to skin at a dose of 2 mg/cm(2). After a 24-h exposure, the skin surface was washed to remove unabsorbed peptide. Skin disks were tape stripped to determine the amount of peptide in the stratum corneum. Removal of the stratum corneum layers was verified by confocal microscopy. The epidermis was heat separated from the dermis and each skin fraction was homogenized. Skin penetration of Ac-EEMQRR-amide was measured in skin layers by hydrophilic interaction liquid chromatography with tandem mass spectrometry using electrospray ionization (ESI) in the positive mode. Stable isotopically labeled hexapeptides were used as internal standards for the quantitation of native hexapeptides to correct for matrix effects associated with ESI. The results (percent of applied dose) showed that the majority of the Ac-EEMQRR-amide was washed from the surface of both HGP and human skin. Ac-EEMQRR-amide that penetrated skin remained mostly in the stratum corneum of HGP (0.54%) and human (0.22%) with the peptide levels decreasing as each layer was removed by tape stripping. Total Ac-EEMQRR-amide found in the epidermis of HGP and human skin was similar at 0.01%. No peptide was detected in the dermis or buffer collected underneath the skin for both human and HGP. There was no hexapeptide metabolite (H2N-EEMQRR-amide) detected in any layers of HGP skin, human skin or buffer collected underneath the skin. This skin penetration data will be useful for evaluating the safety of cosmetic products containing small peptide cosmetic ingredients.

Links

Publisher Full Text (DOI)

Authors+Show Affiliations

Kraeling ME
US Food and Drug Administration, CFSAN/Office of Applied Research and Safety Assessment , Division of Toxicology, Laurel, MD , USA and.
Zhou W
No affiliation info available
Wang P
No affiliation info available
Ogunsola OA
No affiliation info available

MeSH

AnimalsChromatography, LiquidCosmeticsGuinea PigsHumansIn Vitro TechniquesOligopeptidesSkinSkin AbsorptionTandem Mass Spectrometry

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24754410

Citation

Kraeling, Margaret E K., et al. "In Vitro Skin Penetration of Acetyl Hexapeptide-8 From a Cosmetic Formulation." Cutaneous and Ocular Toxicology, vol. 34, no. 1, 2015, pp. 46-52.
Kraeling ME, Zhou W, Wang P, et al. In vitro skin penetration of acetyl hexapeptide-8 from a cosmetic formulation. Cutan Ocul Toxicol. 2015;34(1):46-52.
Kraeling, M. E., Zhou, W., Wang, P., & Ogunsola, O. A. (2015). In vitro skin penetration of acetyl hexapeptide-8 from a cosmetic formulation. Cutaneous and Ocular Toxicology, 34(1), 46-52. https://doi.org/10.3109/15569527.2014.894521
Kraeling ME, et al. In Vitro Skin Penetration of Acetyl Hexapeptide-8 From a Cosmetic Formulation. Cutan Ocul Toxicol. 2015;34(1):46-52. PubMed PMID: 24754410.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - In vitro skin penetration of acetyl hexapeptide-8 from a cosmetic formulation. AU - Kraeling,Margaret E K, AU - Zhou,Wanlong, AU - Wang,Perry, AU - Ogunsola,Oluwatosin A, Y1 - 2014/04/22/ PY - 2014/4/24/entrez PY - 2014/4/24/pubmed PY - 2015/12/25/medline KW - Acetyl hexapeptide-8 KW - peptide KW - skin penetration SP - 46 EP - 52 JF - Cutaneous and ocular toxicology JO - Cutan Ocul Toxicol VL - 34 IS - 1 N2 - There is a concern that peptides in cosmetic creams marketed as anti-aging/anti-wrinkle may penetrate into the deep layers of the skin and potentially stimulate biological activity. Claims for one cosmetic peptide, acetyl hexapeptide-8 (Ac-EEMQRR-amide), suggest interference with neuromuscular signaling as its anti-wrinkle mechanism of action. Therefore, the skin penetration of commercially available Ac-EEMQRR-amide from a cosmetic formulation (oil-in-water (O/W) emulsion) was determined in hairless guinea pig (HGP) and human cadaver skin assembled into in vitro diffusion cells. An O/W emulsion containing 10% Ac-EEMQRR-amide was applied to skin at a dose of 2 mg/cm(2). After a 24-h exposure, the skin surface was washed to remove unabsorbed peptide. Skin disks were tape stripped to determine the amount of peptide in the stratum corneum. Removal of the stratum corneum layers was verified by confocal microscopy. The epidermis was heat separated from the dermis and each skin fraction was homogenized. Skin penetration of Ac-EEMQRR-amide was measured in skin layers by hydrophilic interaction liquid chromatography with tandem mass spectrometry using electrospray ionization (ESI) in the positive mode. Stable isotopically labeled hexapeptides were used as internal standards for the quantitation of native hexapeptides to correct for matrix effects associated with ESI. The results (percent of applied dose) showed that the majority of the Ac-EEMQRR-amide was washed from the surface of both HGP and human skin. Ac-EEMQRR-amide that penetrated skin remained mostly in the stratum corneum of HGP (0.54%) and human (0.22%) with the peptide levels decreasing as each layer was removed by tape stripping. Total Ac-EEMQRR-amide found in the epidermis of HGP and human skin was similar at 0.01%. No peptide was detected in the dermis or buffer collected underneath the skin for both human and HGP. There was no hexapeptide metabolite (H2N-EEMQRR-amide) detected in any layers of HGP skin, human skin or buffer collected underneath the skin. This skin penetration data will be useful for evaluating the safety of cosmetic products containing small peptide cosmetic ingredients. SN - 1556-9535 UR - https://www.unboundmedicine.com/medline/citation/24754410/In_vitro_skin_penetration_of_acetyl_hexapeptide_8_from_a_cosmetic_formulation_ DB - PRIME DP - Unbound Medicine ER -