TY - JOUR T1 - Enhanced skin permeation of a novel peptide via structural modification, chemical enhancement, and microneedles JF - bioRxiv DO - 10.1101/2020.10.07.312850 SP - 2020.10.07.312850 AU - Jungen Chen AU - Junxing Bian AU - Basil M. Hantash AU - David E. Hibbs AU - Chunyong Wu AU - Lifeng Kang Y1 - 2020/01/01 UR - http://biorxiv.org/content/early/2020/10/08/2020.10.07.312850.abstract N2 - Hyperpigmentation is a common skin condition with serious psychosocial consequences. Decapeptide-12, a novel peptide, has been found to be safer than hydroquinone in reducing content of melanin, with efficacy up to more than 50% upon 16 weeks of twice daily treatment. However, the peptide suffers from limited transcutaneous penetration due to its hydrophilicity and large molecular weight. Therefore, decapeptide-12 was modified by adding a palmitate chain in an attempt to overcome this limitation. We also tested the effects of chemical penetration enhancers and microneedles to deliver two peptides through skin. Enhanced skin permeation was found using an in vitro human skin permeation model. Moreover, we examined peptide retention of different formulations in skin. Our data showed that palm-peptides in microneedle patch was the most effective.Competing Interest StatementThe authors have declared no competing interest. ER -