EFFECTIVE IN ONLY 15 DAYS
PHARMACEUTICAL QUALITY
DESCRIPTION
The first hexapeptide that is a mimic of the N-terminal end of SNAP-25 which competes with this protein for a position in the SNARE complex. Argireline® is an alternative to Botulinum Toxin, topically targeting the same wrinkle-formation mechanism in a very different way.
APPEARANCE
Transparent solution containing 0.05% active ingredient.
INCL
Water (Aqua), Acetyl Hexapeptide-8.
PROPERTIES
A unique antio-wrinkle peptide that has been shown in significant testing to be effective against the development of skin wrinkling, being a topical aleternative to Botulinum Toxin A.
APPLICATIONS
Argireline® can be incorporated in cosmetics formulations where removal of the deep lines or wrinkles in the forehead or around the eye area is desired.
SCIENCE
One of the most striking signs of skin agiing is increased wrinkling of the face. This can occur naturally over time and is identified by certain biochemical, histological and physiological changes that are amplified by environmental exposure and other secondary factors as the pull ofgravity or repeated facial movements caused by the contraction of the muscles of facial expression. Muscles are contracted when they receive neurotransmitter release from inside a vesicle.
Argireline® mimics the N-terminal end of SNAP-25 and it competes with the natural protein for a position in the SNARE complex. If the SNARE complex is slightly destabilized, the vesicle can not release neurotransmitters efficeintly and therefore muscle contraction is attenuated, preventing the formation of lines and wrinkles.
DOSAGE
3-10%
SOLUBILITY
Water soluble.
In Vitro Action Mechanism
MUSCLE CONTRACTIONs
The neurotransmitter involved in muscle contraction is acetylcholine and it is released from a
vesicle into the synapse. The SNARE protein complex is formed by three proteins: VAMP,
Syntaxin, and SNAP-25 and it is essential for neurotransmitter release at the synapsis and
mediates the final steps of exocytosis. This complex is like a cellular hook that captures vesicles
and brings them close to the membrane to enable their fusion.
BOTULINUM TOXIN A
Botulinum Toxin A paralyses the mucle by selectively blocking acetylcholine release at the neuromuscular junction. BoNT-A cleaves the protein SNAP-25 irreversibly, and therefore the SNARE complex cannot assemble. The nerve signal cannot be relayed, the muscle cannot contract and it is paralysed.
ARGIRELINE®
Argireline® is a mimic of the N-terminal end of SNAP-25 and it competes with the natural protein
for a position in the SNARE complex, so it destabalizes its formation, without breaking any of its
components. If the SNARE complex is slightly destabalized, the vesicle cannot release
neurotransmitters. As a consequence, muscle contraction is attenuated and the muscle is
relaxed.
In Vitro Action Mechanism
MODULATION OF GLUTAMATE RELEASE IN A NEURON CELL CULTURE
Inhibition of glutamate release by depolarized neuron cells is a validated cell assay for
measuring the potential activity of compounds on the inhibition of neuronal exocytosis.
Untreated neuron cultures were used as a negative control and cultures treated with
Botulinum Toxin A (BoNT-A) were used as a positive control.
In Vivo Efficacy
DETERMINATION OF EFFICACY AGAINST SKIN WRINKLING
This study was carried out in 10 healthy women volunteers. An O/W emulsion containing 10% Argireline® solution was applied twice daily around the eyes for 30 days. Silicon imprints were obtained pre-test and after 15 and 30 days. Analysis of the imprints were performed by confocal v laser scanning microscopy.
0 Days
A cream containing 5% Argireline® solution was applied twice daily around the eyes of 14 volunteers, aged 39 to 64 for 28 days. Silicon imprints of the treated areas were measured by confocal profilometry.
Argireline shows a high inhibitory potential of glutamate release
The inhibition of glutamate release at mM
concentration is a clear indicator of the
potent anti-expression wrinkle activity of
this hexapetide.
Reduction in the depth of
wrinkles up to 17% after
15 days with 10% Serutox
Solution
The depth of the furrow
decreased a maximum
value of 32% in 28 days
* Argireline ® is a registered Trademark of
Lipotec Group Barcelona, Spain. All images and
content used with permission from Lipotec