Human skin penetration of a copper tripeptide in vitro as a function of skin layer.
OBJECTIVE
Skin retention and penetration by copper applied as glycyl-L-histidyl-L-lysine cuprate diacetate was evaluated in vitro in order to assess its potential for its transdermal delivery as an anti-inflammatory agent.


METHODS
Flow-through diffusion cells with 1 cm(2) exposure area were used under infinite dose conditions. 0.68% aq. copper tripeptide as permeant was applied on isolated stratum corneum, heat-separated epidermis and dermatomed skin and receptor fluid collected over 48 h in 4 h intervals using inductively coupled plasma mass spectrometry to analyze 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 97 ± 6.6 μg/cm(2) were retained as depot.


CONCLUSIONS
Copper as tripeptide was delivered in potentially therapeutically effective amounts for inflammatory disease.
Hostynek
Jurij J
JJ
Department of Dermatology, UCSF School of Medicine, San Francisco, CA, USA. jurij.hostynek65@gmail.com
Dreher
Frank
F
Maibach
Howard I
HI
D000085:Acetates / Q000737:chemistry / Q000494:pharmacology; D000279:Administration, Cutaneous; D000328:Adult; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology; D003300:Copper / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D008297:Male; D008875:Middle Aged; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D010539:Permeability; D012867:Skin / Q000033:anatomy & histology* / Q000187:drug effects*; D055815:Young Adult
D000085:Acetates; D000893:Anti-Inflammatory Agents; D009842:Oligopeptides; D003300:Copper