Abstract
Wrinkles can have a negative effect on quality of life and Botox is one of the most effective and common treatments. Argireline (Arg0), a mimetic of Botox, has been found to be safer than Botox and effective in reducing wrinkles, with efficacies up to 48% upon 4 weeks of twice daily treatment. However, the skin permeation of Arg0 is poor, due to its large molecular weight and hydrophilicity. Arg0 exists in zwitterionic form and this charged state hindered its skin permeation. Chemical modification of the peptide structure to reduce the formation of zwitterions may result in increased skin permeability. We investigated a total of 4 peptide analogues (Arg0, Arg1, Arg2, Arg3), in terms of skin permeation and wrinkle reduction. The 4 peptides were dissolved in various propylene glycol and water co-solvents. Enhanced human skin permeation was demonstrated by both Arg2 and Arg3 in vitro. On the other hand, the abilities of the 4 analogues to reduce wrinkle formation were also compared using primary human dental pulp stem cells derived neurons. By measuring the inhibition of glutamate release from the neurons in vitro, it was shown that Arg3 was the most effective, followed by Arg1, Arg0 and Arg2.
Highlights
Wrinkles can have a negative effect on quality of life and Botox is one of the most effective and common treatments
Out of the 3 modified peptide analogues, Arg[2] and Arg[3] had consistently greater cumulative amount of peptides permeated through the skin after 24 hrs, while Arg[1] had consistently less cumulative amount of peptide permeated through the skin after 24 hrs, as compared to Arg[0]
Peptide analogues dissolved in propylene glycol (PG) demonstrated higher amount permeated through the skin
Summary
Wrinkles can have a negative effect on quality of life and Botox is one of the most effective and common treatments. Argireline (Arg0), a mimetic of Botox, has been found to be safer than Botox and effective in reducing wrinkles, with efficacies up to 48% upon 4 weeks of twice daily treatment. Arg[0] competes with SNAP-25 for the binding with vesicle-associated membrane protein (VAMP) This destabilises the formation of a ternary Soluble N-ethylmaleimide-sensitive factor Attachment protein REceptor (SNARE) complex resulting in the inhibition of neuronal exocytosis. Arg[0] has been found to be effective in reducing wrinkles, with efficacies up to 48% upon 4 weeks of twice daily treatment[6,8,9,10]. The poor skin permeation can lead to a significant wastage of peptide, resulting in unwanted high cost of production and an ineffective final dosage form. Hoppel et al showed a clear superiority of water-rich water-in-oil-in-water www.nature.com/scientificreports/
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
