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Cited by 22Advancements in Transdermal Drug DeliveryContact Dermatitis and AllergiesDermatology and Skin Diseases

Human skin retention and penetration of a copper tripeptide in vitro as function of skin layer towards anti-inflammatory therapy

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Hostynek, Jurij J., Dreher, Frank, Maibach, Howard I.·2010·Inflammation Research
DOI 10.1007/s00011-010-0214-4PMC PMC2945467
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Abstract

OBJECTIVE AND DESIGN: The skin retention and penetration characteristics of copper applied as glycyl-L-histidyl-L-lysine cuprate diacetate were evaluated in vitro in order to assess the potential for its transdermal delivery as anti-inflammatory agent. MATERIALS AND METHODS: Flow-through diffusion cells with 1 cm(2) exposure area were used under infinite dose conditions. 0.68% aq. Copper as a tripeptide was applied on isolated stratum corneum, on heat-separated epidermis and on dermatomed skin. Receptor fluid collected over 48 h in 4 h intervals was analyzed by inductively coupled plasma mass spectrometry for copper in tissues and receptor fluid. RESULTS: The permeability coefficient of the compound through dermatomed skin was 2.43 ± 0.51 × 10(-4) cm/h; 136.2 ± 17.5 μg/cm(2) copper permeated 1 cm(2) of that tissue over 48 h, while 82 ± 8.1 μg/cm(2) of copper were retained there as depot. CONCLUSIONS: Applied tansdermally as the tripeptide on human skin ex vivo, copper permeated the skin and was also retained in skin tissue in amounts potentially effective for the treatment of inflammatory diseases.

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  • When 0.68% GHK-Cu was applied to dermatomed skin, 136 micrograms of GHK-Cu passed through the skin per centimeter squared over 48 h.

    “When tested by Howard Maibach’s group (Univerisity of California at San Francisco), 0.68% GHK-Cu was applied to dermatomed skin. Over 48 h, 136 micrograms of GHK-Cu passed through the skin per centimeter squared.”

    From The Effect of the Human Peptide GHK on Gene Expression Relevant to Nervous System Function and Cognitive Decline (2017) · cites this paper as [101]

    The Experimental design section reports applying a 0.68% aqueous GHK-Cu solution, and Results (Table 2) reports 136.2 ± 17.5 μg/cm² in receptor fluid after 48 hours with dermatomed skin. But Table 2 identifies that measured amount as copper, not GHK-Cu; the Materials section also says concentrations are reported in terms of copper. (LLM, conf=0.91)

    Experimental — accuracy not yet measured

  • Studies of GHK passage through the skin by Howard Maibach's laboratory suggest that it may be possible to pass an adequate amount of GHK-Cu through the skin to reduce anxiety, and possibly pain.

    “Studies of GHK passage through the skin by Howard Maibach’s laboratory suggest that it may be possible to easily pass an adequate amount of GHK-Cu through the skin to reduce anxiety, and possibly pain [56].”

    From Regenerative and Protective Actions of the GHK-Cu Peptide in the Light of the New Gene Data (2018) · cites this paper as [56]

    The Results and Discussion (page numbers not provided) report GHK-Cu penetration through human skin ex vivo and estimate that topical delivery could make copper available systemically. The Conclusions describe the dose as potentially therapeutic for anti-inflammatory treatment, but the paper does not establish an amount adequate to reduce anxiety or pain, or show that delivery would be easy in vivo. (LLM, conf=0.88)

    Experimental — accuracy not yet measured

  • A transdermal patch of several centimeters squared may pass therapeutically effective amounts of GHK-Cu throughout the human body.

    “This is a significant amount of GHK-Cu, and a transdermal patch of a several centimeters squared may pass therapeutically effective amounts throughout the human body [101].”

    From The Effect of the Human Peptide GHK on Gene Expression Relevant to Nervous System Function and Cognitive Decline (2017) · cites this paper as [101]

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Research works printed but not linked: 26

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Cited by

Sorted by citations

Authors
Hostynek, J. J., Dreher, F., & Maibach, H. I.
Affiliations
University of California, San Francisco (US)
Venue
Inflammation Research
Publisher
Springer Science and Business Media LLC
Published
2010-08-13
Volume
59
Issue
11
Pages
983-988
ISSN
  • 1023-3830 (ISSN-L)
  • 1420-908X
DOI
10.1007/s00011-010-0214-4
PMC
PMC2945467
OpenAlex
W2023939273
Cited by
22
References
1
Citations by year
2026: 1 · 2025: 3 · 2023: 3 · 2022: 1 · 2018: 3 · 2017: 1 · 2016: 2 · 2015: 5 · 2014: 2 · 2012: 1
FWCI
0.22
Type
journal article
Language
en
Open access
Licence
cc-by-nc
Locations
  • Inflammation Research (publishedVersion, cc-by-nc)
  • PubMed Central (publishedVersion, cc-by-nc)
  • PubMed (publishedVersion)
  • eScholarship (California Digital Library) (submittedVersion)
  • eScholarship (California Digital Library) (submittedVersion, cc-by-nc)
Funders
Università degli Studi di Verona
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
  • Health Sciences › Medicine › Dermatology › Contact Dermatitis and Allergies
  • Health Sciences › Medicine › Dermatology › Dermatology and Skin Diseases
Keywords
copper, transdermal drug delivery, skin permeation, skin retention, stratum corneum, epidermis, anti-inflammatory therapy
MeSH terms
Administration, Cutaneous, Anti-Inflammatory Agents, Cadaver, Copper, Diffusion, Humans, Inflammation, Oligopeptides, Permeability, Skin, Skin Diseases, Molecular Structure

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