Objective To determine the anti-tumor effect of the novel docetaxel (DOC) loaded transferrin modified liposome (DOC-TF-LP) on rat glioma cell line C6. Methods LP

was prepared by film-ultrasonic method. Cellular uptake by brain capillary endothelial cells (bEnd.3) and C6 glioma cells was observed by fluorescence quantitative experiment. The anti-proliferation efficiency of DOC-TF-LP was evaluated by MTT assay. Tumor spheroids were used to evaluate the targeting efficiency and anti-tumor ability of DOC-TF-LP. Results Efficiency of TF-LP cellular uptake by C6 glioma cells was 3.2 times of LP (P<0.05). Efficiency of TF-LP cellular uptake by bEnd.3 was 2.6 times of LP (P<0.05). The anti-proliferative activity of DOC-TF-LP were higher than those of DOC-LP and DOC (P<0.05). Fluorescence intensity of TF-LP was higher than that of LP after incubation with C6 tumor spheroids. Gross tumor volumes decreased to 80%, 65%, and 38% after incubation with DOC, DOC-LP, and DOC-TF-LP, respectively. Conclusion Compared to DOC and DOC-LP, DOC-TF-LP could more persistently inhibit the proliferation of C6 cells and C6 tumor spheroids. Thus, DOC-TF-LP, as a new nanometer drug, has a special application value for the therapy of glioma.