초록 |
Hydroxy-terminated methoxy poly(ethylene glycol)(MePEG)/poly(ε-caprolactone)(PCL) amphiphilic block copolymers were synthesized by a ring opening polymerization of ε-caprolactone in the presence of MePEG homopolymer without any catalysts. Hydroxy-terminated MePEG/PCL was converted into a primary amino-terminated MePEG/PCL. Folate conjugated MePEG/PCL were synthesized by a coupling of folic acid to MePEG-PCL-NH2. Using these diblock copolymers, we have prepared Paclitaxel-loaded polymeric nanospheres by micelle formation. The chemical composition of the copolymer was characterized by 1H-NMR, GPC, and UV spectroscopy. The yield of folate conjugation was about 70~80%. The size of nanospheres exhibited a narrow monodisperse size distribution and average particular diameters less than 150 nm. The nanosphere had a relatively high drug loading efficiency. To elucidate the relation between the folate receptors and nanospheres, paclitaxel containing fluorescence was prepared and their uptake was detected in MCF-7 breast carcinoma cells using confocal laser scanning microscopy. This approach is expected to be useful for effective tumor cell-selective targeting. |