The objective of this study is to evaluate -in vitro and in vivo- the biocompatibility , antitumor avticity and tumor targeting of Tf-coated BCNU-loaded Poly(D,L-lacticAcid) (PLA) nanoparticles (Tf-BCNU-PLA-NPs) against C6 Glioma cells. The nanoparticles were provided and characteristics were studied by the College of Material and Engineering of Tianjin University who reported the size of NPs as 100~200nm. Our study includes two parts.The first part "In vitro study": Particiles were prepared with spontaneous emulsification /solvent extraction method. SEM showed that nanoparticles with small particle size and narrow size distribution, which had spherical geometry had been acquired. Bratton-Marshall colorimetric method was used to determine the drug content and the influence of initial BCNU content, molecular weight of PLA on drug encapsulation efficiency were evaluated. The Study of in vitro drug release behavior demonstrated that BCNU-loaded PLA nanoparticles had shown certain sustained release characteristics. Particles with low molecular weight of PLA showed higher burst effect and significantly faster release of drug from PLA samples. The results of MTT cytotoxicity test significantly demonstrated that drug-loaded nanoparticles had higher antitumor activity comparing with free BCNU group, and sustained drug release character was achieved as well. In addition, empty nanoparticles demonstrated that the matrix had low cytotoxicity and therefore a good biocompatibility. For evaluating the tumor targeting of the Tf-coated BCNU-loaded Poly(D,L-lacticAcid) (PLA) nanoparticles (Tf-BCNU-PLA-NPs) in vitro,we used Fluorescent labeling of nanoparticles method, targeting of effect of (Tf-BCNU-PLA-NPs) was observed by Olympus phase-contrast fluorescent microscopy at defined time intervals and recorded by Olympus microscopy. Results showed that .after labeling by FITC, the (Tf-BCNU-PLA-NPs) gathered at margin of glioma cells within 4 hours detected by fluorescent phase-constract microscopy, then profiled the glioma cells at 12 to 24 hours. While the BSA-coated nanoparticles "used as control group" gathered at the margin of C6 glioma cells after 12 hours, and profiled glioma cells after 24 hours.The second part "In vivo study": For further evaluation of the biocompatibility, antitumor activity and tumor targeting of the nanoparticles ,the in vivo study was carried out using established intracranial glioma-bearing rats. The results demonstrated that (Tf-BCNU-PLA-NPs) had a good biocompatibility , a comparable stronger cytotoxicity by prolonging the mean survival time of rats and a good tumor targeting as well, especially when treated at the early time with higher dosage of BCNU, the average survival time of rats treated stereotacticly was prolonged up to 88.37%, furthermore ,one rat kept normal behavior continuously up to 60 days of observation period. Moreover, another study of different ways of giving (Tf-BCNU-PLA-NPs) to tumor-bearing rats including intracarotid injection and stereotactic and comparing them with BCNU-PLA disc implants demonstrated the ability of the particles to penetrate BBB and access anitumor activity and tumor targeting.