The Efficiency and Safety of Leuphasyl—A Botox-Like Peptide

Abstract

Peptides of synthesis are a very new strategy in cosmetic science and technology for at least two reasons: (1) they are small molecules, easily penetrable in the skin and (2) they are able to induce a very specific action, because all skin cells (keratinocytes, fibroblasts, nervous cells) have membrane receptors for peptides. This group of cosmeceutics includes the botox-like peptides, represented by acetyl hexapeptide 3 (Argireline) and pentapeptid-3 (Leuphasyl). The latter is less known and has been less studied. This substance inhibits the neuromuscular synapses in the mimic muscles, acting as enkephalins. It links the enkephalin receptor to nervous cells, thereby modulating the release of acetylcholine in synaptic space. This cellular activity will be translated in vivo in a relaxation of the muscle and a reduction of expression wrinkles. The aim of our study is to evaluate the optimal concentration of Leuphasyl for skin application at the mimic muscle level, the efficiency and the safety of this peptide. We formulated three emulsions of different concentrations (0.5%, 1%, 2%) which were applied to the skin, at the level of mimic muscles (1) at the eyebrows zone (above the corrugator supercilii muscle) and (2) at the periorbital zone (above the orbicularis oculi muscle). We evaluated the regression of the wrinkles between the eyebrows using an imagistic method: pro-derm Analyser. The study is of interest to discussions concerning how to apply these kinds of cosmetic products at the mimic muscle skin level and not at the level of the wrinkles.

The efficacy study of the combination of tripeptide‐10‐citrulline and acetyl hexapeptide‐3. A prospective, randomized controlled study

“…The significant results were obtained for the frontal region compared with periorbital region. A possible explanation is that for the periorbital region, a big group of muscle fibers is involved ( orbicularis oculi ) but at the intereyebrows zone level there is only one important mimic muscle ( corrugator supercilii ) …”

“…The combination of active ingredients with different or same mode of action such as of growth factor with antioxidants or acetyl hexapeptide‐3 with a botox‐like peptide, that is, pentapeptide‐3 for the enhancement of the anti‐aging effects, and the possible synergy is a new trend in the cosmetic industry.…”

D-tyrosine adds an anti-melanogenic effect to cosmetic peptides

“…1). We selected Leuphasyl (pentapeptide-18; YdAGFL), a commercialized cosmetic peptide that acts as a neurotransmitter inhibitor to reduce fine lines and wrinkles 19,20 . We synthesized pentapeptide-18 peptides in which we either replaced L-tyrosine with D-tyrosine at the N-terminus or added a L-or D-tyrosine at the C-terminus ( Fig.…”

“…For instance, palmitoyl oligopeptide and acetyl hexapeptide-3 are used for collagen stimulation, wound healing, "Botox-like" wrinkle smoothing, and whitening effects 27 . Pentapeptide-18 is a neurotransmitter-inhibiting peptide that decreases neuronal activity and catecholamine release 28 , giving it Botox-like effects in reducing fine lines and wrinkles, and improving firmness 20 . Therefore, in terms of commercial applications, D-tyrosine-modified peptides hold more promise than D-tyrosine as a free amino acid.…”

Topical Peptide Treatments with Effective Anti-Aging Results

“…Three concentrations (0.5%, 1%, and 2%) of Leuphasyl formulations were applied on 20 volunteers for two months, at the level of mimic muscles in the eyebrows zone and in the periorbital zone [48]. To further evaluate anti-wrinkle effects, an in vivo study with 22 females with an average age of 51, was designed.…”