5-Fluorouracil (5-FU) and antisense-EGFR cDNA loaded nanoparticles were prepared by improved W/O/W method using poly (D

L-lactide-co-glycolic acid) (PLGA) and

O

-carboxymethyl chitosan (O-CMC) due to their attractive degradation and physicochemical properties

and this multiple-functional drug delivery system can realize the combination effect of anticancer drug and gene in the therapy of diseases.The results of characterizing these nanoparticles showed that:the mean size

polydispersity and Zeta potenial of 5- FU-encapsulated PLGA/

O

-CMC NPs while absorbing antisense-EGFR was 258.7nm

0.142

and -10.67eV

respectively.The release behavior of 5-FU and gene from NPs was coincidence with Zero-level release. Gliomas cell viability in vitro as well as immunohistochemical staining demonstrated that these nanoparticles had high cytotoxicity on gliomas cells TJ905.Fluorescence confocal microscope was used to trace the procedures of cell transfection induced by nanoparticles.It was found that nanoparticles were both in cytoplasma and nucleus after 24h.