Self-Assembled Skin-Penetrating Peptides with Controlled Supramolecular Properties for Enhanced Transdermal Delivery

Abstract

The use of nanocarriers decorated with penetrationenhancing agents (PEAs) is considered to be a promising approach for efficient transdermal delivery. In this study, we developed short amphiphilic skin-penetrating peptides (17 amino acids) that functioned not only as PEAs but also as building blocks of nanocarriers without the incorporation of additional macromolecules for self-assembly and guest molecule encapsulation. Interestingly, varying only two amino acids in the hydrophobic moiety of the peptides resulted in significantly different selfassembly behavior, thermal stability, protease resistance, and skinpenetration efficiency in a human skin model. The analysis of the peptide secondary structure revealed that such characteristic changes arose due to the sequence variation-mediated conformational change in the hydrophobic block. These findings hold significant promise for the development of simple and effective delivery systems exhibiting controllable supramolecular properties.

Progress in Topical and Transdermal Drug Delivery Research—Focus on Nanoformulations

“…Confocal microscopy showed higher levels in the dermis (4.4-, 18.8-, and 32.9-times higher than the control), emphasizing the potential of CPP-conjugation for transdermal delivery of macromolecular drugs. In another recent approach, Kang et al [ 189 ] developed functionalized nanocarriers with CPPs for enhancement of transdermal delivery. The basic vehicles exhibited specific self-assembly and penetration efficiency in dependence of their amino acid composition, indicating that tailor-made vehicles can be designed for delivery of different actives.…”