Supramolecular Assembly System for Transdermal Penetration of Self-Assembled Short Peptides.

Transdermal delivery of peptides and proteins remains a challenge in the field of drug delivery. In this study, we successfully prepared a series of bio-based ionic liquids by proton exchange reaction adopting green-sourced organic acids and alkaloids as precursors. In addition, we constructed a supramolecular assembly system by taking advantage of self-assembled short peptides (specifically, a custom amphiphilic sequence RRIIIIRR). We also optimized the basic properties of the ionic liquid by a combination of electron microscopy and simulation computation techniques, and the transdermal absorption efficiency of the self-assembled short peptide was successfully increased by 3-fold with the benefit of the pro-permeability properties. Furthermore, cell-level experiments demonstrate that the supramolecular assembly system not only maintains the activity of the self-assembled short peptide but also brings unexpected synergistic amplification effects. In conclusion, this creative system is simple, green, and safe, which can contribute to the application of peptides as well as the interdisciplinary crossover cooperations.