A novel biodegradable amphiphilic copolymer composed of hydroxypropyl-β-cyclodextrin, polylactide, and 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine, was successfully synthesized. The chemical structures of copolymers were determined by FT-IR, (1)H nuclear magnetic resonance (NMR) spectroscopy, (13)C NMR, (31)P NMR, thermogravimetric analysis ,and differential scanning calorimetry. Doxorubicin (DOX)-loaded copolymer nanoparticles (NPs) were prepared by double emulsion and nanoprecipitation methods. The factors of copolymer composition and fabrication methods, which influence size and encapsulation efficiency (EE) were investigated. Their EE to DOX could reach 90.6% at an available condition. In vitro release behavior of NPs showed a continuous release after a burst release. The antitumor activity of the DOX-loaded NPs against cancer HepG2 and A549 cells was evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide method. The DOX-loaded copolymer NPs showed comparable anticancer efficacy with the free drug.
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