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

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. Arginine-α,β-dehydrophenylalanine (RΔF) was synthesized using solution-phase synthesis which self-assembled into nanospheres. Van was entrapped in the nanoparticles (NPs). and efficacy of Van-RΔF was determined using broth microdilution and the mouse thigh infection model, respectively. Van-RΔF NPs efficiently inhibited bacterial growth (), while Van alone showed limited growth inhibition in . Intravenous administration of Van-RΔF in mice with bacterial thigh infection showed enhanced efficacy (double) compared with Van alone, which indicates its high potential for further development.