Development of transferrin functionalized poly(ethylene glycol)/poly(lactic acid) amphiphilic block copolymeric micelles as a potential delivery system targeting brain glioma.
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.
School of Materials Science and Engineering, Tianjin University, Tianjin, 300072, China.
Wei-hua
WH
Ren
Jiang
J
Chang
Cheng-hu
CH
Yan
Xiao-min
XM
Qian
Li-xia
LX
Long
Bin
B
He
Xu-bo
XB
Yuan
Chun-sheng
CS
Kang
Didier
D
Betbeder
Jing
J
Sheng
Pei-yu
PY
Pu
D001932:Brain Neoplasms / Q000188:drug therapy*; D005910:Glioma / Q000188:drug therapy*; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008823:Micelles; D011092:Polyethylene Glycols / Q000737:chemistry*; D014168:Transferrin / Q000737:chemistry*
D008823:Micelles; D014168:Transferrin; D019344:Lactic Acid; D011092:Polyethylene Glycols