Abstract:Objective To prepare the paclitaxel-loaded poly(2-oxazolyl) nano-micelles and to investigate the morphological changes of nano-micelles after changing drug dosage, so as to establish a novel block copolymer micelles delivery system with high loading capacity. Methods The paclitaxel-loaded poly(2-oxazolyl) nano-micelles were prepared using filming-rehydration method. The physical and chemical properties of the prepared nano-micelles, including particle size, encapsulation efficiency and drug loading efficiency, were characterized. The in vitro release characteristics of the prepared nano-micelles were investigated by membrane dialysis method, and the cytotoxicity was determined by CCK-8 method. Results The morphology of micelles gradually extended from spherical to worm-like when the mass ratio of paclitaxel and poly(2-oxazoline) increased from 80:100 to 110:100. The particle size, encapsulation efficiency and drug loading efficiency of spherical micelles were (43.17±0.95) nm, (88.81±2.93)% and (40.49±2.03)%, respectively, while those of worm-like micelles were (107.83±1.51) nm, (77.08±0.97)% and (40.34±0.51)%, respectively. The 24 h cumulative release rates of spherical micelles and worm-like micelles in PBS were (76.58±3.07)% and (77.66±1.00)%, respectively; meanwhile, those in PBS with 2% bovine serum albumin were up to (100.31±1.80)% and (99.73±2.56)%, respectively. The IC50 values of sphere micelles and worm-like micelles on human lung adenocarcinoma cell line A549 were 0.336 μg/mL and 0.342 μg/mL, respectively. Conclusion Paclitaxel-loaded spherical micelles and worm-like micelles with high loading capacity have been successfully prepared. In vitro cytotoxicity Results have found that both micelles have anti-tumor activities.