2024 Volume 73 Issue 11 Pages 1411-1422
In this study, the effects of incorporating arginine-modified peptide into the structure of discshaped bicelles were investigated. Characterization of bicellar system was conducted using different techniques, including dynamic light scattering (DLS), zeta potential, cryogenic transmission electron microscopy (cryo-TEM) and small angle X-ray scattering (SAXS). Bicelle skin permeability as drug carriers was also evaluated. The addition of peptides revealed formation of small-sized, stable and discoidal-shaped bicelles. Positive zeta potential and synchrotron radiation experiments confirmed the presence and showed the peptide distribution across the bicelle face and rim region. A major disruption with the lipid rearrangement of the stratum corneum and the disruption of bicelle structures by the interaction between bicelle lipids and stratum corneum lipids were observed during the application of bicelles with cholesteryl chloroformate-arginine 8-mer (CholR8). This also demonstrated the highest penetration of the drug-loaded bicelle across the hairless mouse skin. As a model drug, non-steroidal anti-inflammatory drug, meloxicam was selected. Meloxicam was incorporated into the hydrophobic domain of bicelles due to its hydrophobic property. Considering these results, bicelle induced with peptides exhibits useful and promising characteristics and behaviors, shaping an effective strategy for future transdermal drug delivery applications.
