Conformationally restricted, dipeptide-based, self-assembled nanoparticles for efficient vancomycin delivery - supplementary dataset

Aim: Emergence of vancomycin (Van) resistance, and usage of its higher dose and short half-life are
posing a serious concern. Slow and sustained release of Van using a nanodelivery system may overcome
these problems. Materials & methods: Arginine-α,β-dehydrophenylalanine (R?F) was synthesized using
solution-phase synthesis which self-assembled into nanospheres. Van was entrapped in the nanoparticles
(NPs). In vitro and in vivo efficacy of Van-R?F was determined using broth microdilution and the mouse
thigh infection model, respectively. Results & conclusion: Van-R?F NPs efficiently inhibited bacterial
growth (Staphylococcus aureus), while Van alone showed limited growth inhibition in in vitro. Intravenous
administration of Van-R?F in mice with bacterial thigh infection showed enhanced efficacy (double)
compared with Van alone, which indicates its high potential for further development.