The serious therapeutic obstacles to
glioma treatment include poor penetration across the blood-brain barrier (BBB) and low accumulation of therapeutic drugs at
tumor sites. In this study,
borneol combined with CGKRK
peptide (a ligand of the
heparan sulfate which overexpress on the
glioma cells) modified
paclitaxel prodrug self-assembled redox-responsive nanoparticles (CGKRK-PSNPs) were hypothesized to enhance the BBB penetration ability and active
tumor targeting efficiency, respectively. The resulting CGKRK-PSNPs possessed a spherical shape with a small particle size (105.61 ± 1.53 nm) and high drug loading for PTX (54.18 ± 1.13%). The drug release behavior proved that CGKRK-PSNPs were highly sensitive to
glutathione (GSH) redox environment. The in vitro cell experiments suggested that CGKRK-PSNPs significantly increased the cellular uptake and cytotoxicity of U87MG cells, meanwhile CGKRK-PSNPs showed the low cytotoxicity against BCEC cells. Combined with
borneol, CGKRK-PSNPs exhibited enhanced transportation across in vitro BBB model. In intracranial U87MG
glioma-bearing nude mice, the higher accumulation of CGKRK-PSNPs combined with
borneol was observed through real-time fluorescence image. Moreover, the in vivo anti-
glioma results confirmed that CGKRK-PSNPs combined with
borneol could improve the anti-
glioma efficacy with the prolonged medium survival time (39 days). In conclusion, the collaborative strategy of CGKRK-PSNPs combined with
borneol provided a promising drug delivery routine for
glioblastoma therapy.