The aim of present study is to conceive a biodegradable poly(
ethylene glycol)-
polylactide (
PEG-PLA) copolymer nanoparticle which can be surface biofunctionalized with
ligands via
biotin-
avidin interactions and used as a potential
drug delivery carrier targeting to brain
glioma in vivo. For this aim, a new method was employed to synthesize biotinylated
PEG-PLA copolymers, i.e., esterification of PEG with biotinyl
chloride followed by copolymerization of hetero-biotinylated PEG with
lactide.
PEG-PLA nanoparticles bearing
biotin groups on surface were prepared by nanoprecipitation technique and the functional
protein transferrin (Tf) were coupled to the nanoparticles by taking advantage of the strong
biotin-
avidin complex formation. The flow cytometer measurement demonstrated the targeting ability of the nanoparticles to
tumor cells in vitro, and the fluorescence microscopy observation of brain sections from C6
glioma tumor-bearing rat model gave the intuitive proof that Tf functionalized
PEG-PLA nanoparticles could penetrate into
tumor in vivo.