Glioma homing peptide-modified PEG-PCL nanoparticles for enhanced anti-glioma therapy

AbstractBackground: Peptide-mediated drug delivery system (DDS) has been increasingly used to promote on-demand treatment efficacy of cancers. Herein, LTLRWVGLMS (LS10) peptide is selected as the functional ligand for specific glioma-targeting drug delivery. LS10 peptide selectively binds to NG2 proteins that are widely overexpressed in the glioma cells and restricted in normal tissue. LS10 peptide-decorated DDS is expected to hold vast promises in glioma therapy and decrease unwanted side effects.Methods: LS10 peptide was conjugated on the surface of poly(ethylene glycol)-poly(ɛ-caprolactone) (PEG-PCL) nanoparticles via 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride/N-hydroxysulfosuccinimide coupling reaction. Using U87MG cells as the glioma cell model, cellular uptake, internalization mechanism, cellular cytotoxicity and apoptosis were investigated. 1,1′-Dioctadecyl-3,3,3′,3′-tetramethyl indotricarbocyanine iodide were used as fluorescence probes to investigated in vivo glioma targeting cap...