Lf modified PSNPs based on HA/CSH/PEG20000 were prepared for targeting brain glioma. Modification efficiency and modified amount of Lf on Lf-Cur-PSNPs were determined. The cellular uptakes of different PSNPs were investigated in BCECs and C6 cells. Ex vivo imaging studies of Lf-PSNPs showed more accumulation in the brain than PSNPs. Dual targeting for BBB and glioma cells could be achieved with Lf-PSNP.