Preparation and characterization of thermosensitive and folate functionalized Pluronic micelles.
In this study, thermosensitive and folate functionalized poly(ethylene oxide)-b-poly(propylene oxide)-b-poly(ethylene oxide)-ploy(N-isopropylacrylamide-co-hydroxyethyl methacrylate) (FA-Pluronic-PNH) copolymer was synthesized. The structure and molecular weight of the copolymer were confirmed by 1H NMR, FT-IR and GPC, respectively. The lower critical solution temperature (LCST) of the copolymer was 39.8 degrees C. By employing doxorubicin (DOX) as a model drug, folate receptor-targeted DOX-loaded micelles were further formed on the copolymer. The blank and DOX-loaded micelles both exhibited nearly spherical shapes and their average diameters were 35 nm and 50 nm, respectively. The in vitro release behaviors of the DOX-loaded micelles were temperature-dependent and the release rate of DOX at 42 degrees C (above LCST) was faster than that at 37 degrees C (below LCST). Furthermore, the cytotoxicity assays of free DOX and DOX-loaded micelles on human cervical cancer cell lines HeLa and human lung cancer cell lines A549 demonstrated that folate increased the cellular uptake of the micelles within targeted cells that vastly over-expressed folate receptors.
Shanghai Key Laboratory of Functional Materials Chemistry, Research Center of Analysis and Test, East China University of Science and Technology, Shanghai 200237, China.
Cheng
C
Yang
Hongli
H
Zhao
Huihui
H
Yuan
Ronghua
R
Yu
Minbo
M
Lan
D002850:Chromatography, Gel; D005492:Folic Acid / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D008823:Micelles; D046529:Microscopy, Electron, Transmission; D020442:Poloxamer / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared
D008823:Micelles; D020442:Poloxamer; D005492:Folic Acid