Glioblastoma is one of the most malignant
brain tumors with a poor prognosis. In this study, we examined the effects of
transferrin (Tf)-modified poly ethyleneglycol-
poly lactic acid (
PEG-PLA) nanoparticles conjugated with
resveratrol (Tf-
PEG-PLA-RSV) to
glioma therapy in vitro and in vivo. The cell viability of Tf-
PEG-PLA-RSV on C6 and U87
glioma cells was determined by the MTT assay. In vivo biodistribution and antitumor activity were investigated in Brain
glioma bearing rat model of C6
glioma by i.p. administration of RSV-
polymer conjugates. We found that the average diameter of each Tf-
PEG-PLA-RSV is around 150 nm with 32 molecules of Tf on surface. In vitro cytotoxicity of
PEG-PLA-RSV against C6 and U87 cells was higher than that of free RSV, and further the modification of Tf enhanced the cytotoxicity of the RSV-
polymer conjugates as a result of the increased cellular uptake of the RSV-modified conjugates by
glioma cells. In comparison with free RSV, RSV conjugates could significantly decrease
tumor volume and accumulate in
brain tumor, which resulted in prolonging the survival of C6
glioma-bearing rats. These results suggest that Tf-NP-RSV had a potential of
therapeutic effect to
glioma both in vitro and in vivo and might be a potential candidate for targeted
therapy of
glioma and worthy of further investigation.