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.