32 LIFESTYLE COSMETICS
Endorphin peptide-based wrinkle treatment
Guglielmo Bifulco, Francesco Rastrelli, Gianbattista Rastrelli, Giorgio Tosti - Kalichem
The cosmetics industry and consumers have been paying increasing attention to the concept of neurocosmetics in recent years. Scientific evidence about the benefits of natural and biomimetic cosmetics substances involved in the modulation of human physiology, mood and state of mind through interaction with the skin nervous system has impacted the industry at unprecedented levels. This scenario led to a new trend for the
use of active ingredients targetting specific nervous system pathways in the skin, such as endocannabinoid and opioid systems. Consumer demand is becoming more challenging, to the point where the actual composition and functional characteristics of the cosmetics products used throughout the daily routine have to be compliant to a specific ‘lifestyle’ model.
Endorphins The endogenous opioid system is one of the most studied innate pain-relieving systems1
. It is very
well known in mass culture for its key role in the physiological ‘endorphin rush’, a brain reaction where the endorphins (the neurotransmitters involved in such a biological opioid pathway) are able to trigger a positive state of mind and feelings such as reduced stress, improved self- esteem, an energised outlook on life and muscle relaxation2
. The endorphin rush is a condition typically
associated with the feelings that people experience after doing regular work-outs, yoga sessions, sexual activity or after accomplishing satisfactory results so as to reach personal goals. The power of endorphins in the collective imagination and consumer mind can be grasped intuitively from its etymology: the word derives from Greek works éndon (meaning ‘within’) and Morpheus, the god of dreams in Greek mythology.
Technology background In this article, we describe a biomimetic endorphin oligopeptide-based complex called
BEFORE Benchmark cream ■ Peptilift cream ■
60 50 40 30 20 10 0
Forehead lines Frown lines
Peptilift (INCI: Sh-Pentaptide-5), which has a particular tropism for the skin’s neuroendocrine system. It is incorporated into a functional lipo-oligopeptidic delivery system based on conjugated linoleic acid (CLA) glutathione (INCI: Potassium Glutathione Isomerised Linoleate), which selectively activates opioid signalling directly on the skin and has intrinsic ‘anti- inflammageing’, detoxifying and anti-pollution properties. The technology is therefore an avant garde solution in line with the neurocosmetic philosophy for anti-ageing care. The synergistic combination of these specialities makes it possible to counteract the main processes underlying skin ageing, including: ■ Contraction of the facial mimic muscles, resulting in the formation of expression wrinkles ■ Microinflammation, which induces oxidative stress and premature ageing (inflammageing) ■ Reduced cell regeneration rates, causing a reduction in the skin barrier function with loss of water, thinning of the skin, elasticity reduction and wrinkle formation The physiology of the skin is finely regulated
by the complex interaction between the immune, endocrine and nervous systems. The skin communicates with the nervous system
AFTER Nasolabial folds Figure 1: Wrinkle volume reduction (%) after 4 weeks: Peptilift v benchmark
through different receptors, including opioid receptors. These receptors are mainly involved in pain control, but they also regulate skin homeostasis, skin regeneration and wound healing3,4
. In particular, δ-opioid receptors (DOPrs) are
able to modulate cell differentiation, migration and proliferation at skin level, while their activation has also been proven to promote the maintenance of the skin barrier function5 and reduce the production of pro-inflammatory mediators. DOPrs therefore represent an important target for anti-ageing treatments6 Indeed, they are less expressed in the
.
skin of elderly subjects than young subjects. Furthermore, reduced DOPr activity is related to earlier ageing, while scientific evidence has highlighted their increased expression in keratinocytes following UV exposure5
. We
may therefore speculate that the activation of DOPrs by an agonist, such as endorphins, may promote skin regeneration, improve skin appearance and reduce the signs of ageing.
Sh-Pentaptide 5 The biomimetic endorphin oligopeptide acts as a presynaptic inhibitor of muscle contraction7
, thus exerting a botox-like activity Figure 2: Wrinkles on volunteer’s forehead before & after 4 weeks of treatment with Peptilift PERSONAL CARE April 2022
for reducing expression wrinkles. By mimicking a physiological mechanism, it inhibits presynatic neuron depolarisation in the neuromuscolar junction. The active binds to presynaptic DOPrs, closing the calcium channels and reducing the release of the excitatory neurotransmitter acetylcholine in the synaptic space. As a result of this interaction, it decreases the face mimic muscle fibres’ contractile response by inducing their relaxation, with a resulting reduction in the onset of expression wrinkles.
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