Abstract

Acute exposure to UV radiations results in erythema, immune suppression and cell death, while chronic exposure results in photoaging and carcinogenesis. In order to fight UV-induced skin damages, we have developed an oil-soluble form of an α-MSH biomimetic peptide. The binding of α-MSH to its melanocortin-1 receptor (MC1-R) induces epidermal pigmentation, which in turn activates the signal transduction pathway leading to the induction of melanin synthesis. In addition, it has been proven that α-MSH directly reduces UV-induced DNA damage and enhances DNA repair in epidermal melanocytes and keratinocytes, by modulating the function of DNA repair molecules. The objective of this study was to investigate whether a biomimetic peptide analogue of α-MSH, acetyl hexapeptide-1, was able to stimulate the natural skin defense system against sun exposure. We demonstrated in vitro that acetyl hexapeptide-1, acts effectively and simultaneously on melanogenesis to improve natural cell UV protection by melanin, on DNA protection (Comet assay, reduction in 8-oxo-dG) and repair (decrease in sunburn cells, caspase-3 activity and pyrimidine dimers) to limit photoaging and on the inflammatory cascade to soothe sun-ravaged skin (IL-1α, IL-8, PGE2 ). Clinically this biomimetic peptide demonstrated its efficacy on the increase in skin pigmentation and anti-erythemal properties after 14 days skin application showing a significant increase (+20%) of the Minimal Erythemal Dose compared to placebo. Furthermore, we developed a smart lipophilization technology (transparent w/o microemulsion) in order to improve the peptide diffusion through the Stratum corneum and allow its introduction in clear oil-based products.Especially designed to be introduced in oil-based products, this peptide represents the biological solution to improve sun care and anti-aging product efficacy in order to limit sun-induced premature aging.

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