Peptide Amphiphile Nanostructures for Targeting of Atherosclerotic Plaque and Drug Delivery

Coassembled peptide amphiphile nanofibers designed to target atherosclerotic plaque and enhance cholesterol efflux are shown to encapsulate and deliver a liver X receptor agonist to increase efflux from murine macrophages in vitro. Fluorescence microscopy reveals that the nanofibers, which display an apolipoprotein-mimetic peptide, localize at plaque sites in low density lipoprotein receptor knockout (LDLR KO) mice with or without the encapsulated molecule, while nanofibers displaying a scrambled, nontargeting peptide sequence do not demonstrate comparable binding. These results show that nanofibers functionalized with apolipoprotein-mimetic peptides may be effective vehicles for intravascular targeted drug delivery to treat atherosclerosis.