Bergamot waste derived lipid nanosystems as novel excipients for (trans)dermal drug delivery

Inedible waste from the bergamot processing industry is typically used to produce essential oil, parfums, pectin etc. Nevertheless, the discarded bergamot peels can still serve as a valuable source of novel lipid ingredients. This study explores the potential of using lipid components from bergamot peels (BLCs) to create lipid-based nanosystems (LBNs) for skin application. BLCs were extracted and characterized by GC/MS and ATR-FTIR. LBNs were prepared by hot melt homogenization, and their ultrastructure was studied by cryo-EM and SAXS. Ibuprofen (IB) was chosen as model drug. The in vitro skin permeation pattern of IB either loaded in LBNs (IB-LBNs) or co-administered with empty LBNs was studied using porcine skin. The LBNs had a mean diameter of about 150 nm and a core-shell structure. LBNs increased the IB flux through porcine skin by a factor of three, both in IB-LBNs form and after co-administration with the free drug solution. This data suggests that BLCs act as skin penetration enhancers rather than drug carriers. ATR-FTIR results further indicated that BLCs perturb the structure of stratum corneum lipids, likely due to the presence of unsaturated fatty acid esters in BLCs extract. In conclusion, BLCs could be promising novel and natural excipients for the design of cutaneous preparations.