To prepare docetaxel/DSPE-PCB 5K formulation, 150 mg of DSPE-PCB 5K and 6 mg docetaxel were co-dissolved in 5 ml trifluoroethanol in a round-bottom flask. The solvent was subsequently evaporated by rotary evaporation to obtain a thin film. The film was then kept in a vacuum for 2 hours at room temperature to remove the residual trifluoroethanol. After the addition of 3 ml saline and stirring at 800 rpm for 30 min, a clear micelle solution with docetaxel loaded was obtained. Docetaxel/DSPE-PEG 5K and docetaxel/Polysorbate 80 formulations were prepared following the same procedure. Taxotere was prepared follow the reference63 (link), 64 (link), 69 . The weight ratios of drug over surfactant for all formulations were kept at 4%, which is the drug loading level for TAXOTERE®66 , 68 (link).
Drug release profiles were determined by placing 100 μL different formulations into Slide-A-Lyzer MINI dialysis microtubes (3500 Da MW cutoff) and dialyzed against PBS at 37°C with gentle stirring. At different time intervals, docetaxel remained in the dialyzer was quantified through HPLC by a Waters Breeze 2 System equipped with a Waters 2998 photodiode array detector at 230 nm and a Waters symmetry C18 column (4.6×7.5 mm). The mobile phase was a mixture of acetonitrile/water (50%:50% volume) at a flow rate of 1 mL/min. The docetaxel showed a single elution peak at 5.47 min.
Drug release profiles were determined by placing 100 μL different formulations into Slide-A-Lyzer MINI dialysis microtubes (3500 Da MW cutoff) and dialyzed against PBS at 37°C with gentle stirring. At different time intervals, docetaxel remained in the dialyzer was quantified through HPLC by a Waters Breeze 2 System equipped with a Waters 2998 photodiode array detector at 230 nm and a Waters symmetry C18 column (4.6×7.5 mm). The mobile phase was a mixture of acetonitrile/water (50%:50% volume) at a flow rate of 1 mL/min. The docetaxel showed a single elution peak at 5.47 min.
