| Objective:To prepare the vincristine sulfate loaded PEG-PLGA nanoparticles(PEG-PLGA-VCR-NPs), evaluate its quality and study its in vitro anti-tumor activity to HepG2 cells.Methods:PEG-PLGA-VCR-NPs was prepared by the double emulsion-solvent evaporation method, the best preparation technician condition was optimized according to orthogonal test based on single-factor test. Quality evaluation as the appearance and its redispersibility, morphous, particle size and its distribution, zeta potential, drug loading, encapsulation efficiency, stability and in vitro drug release, the growth inhibition to HepG2 cells was determined by MTT assay.Results The best preparation technician condition was PEG-PLGA concentration:20mg/mL, the volume ratio of internal water to oil phase: 4/10, external water to oil phase:6/1, ultrasound time:1.5min. PEG-PLGA-VCR-NPs was white, loose powder with good redispersibility, its shape was spherelike, its average diameter was 159.6±2.1%nm, drug loading was 6.54d±1.3%, encapsulation efficiency was 70.5±1.5%, it was stored at 4℃for 6 months with good stability, in vitro drug release experiment showed it exhibited consequently sustained release for 14d, the cumulative release was up to 93.3% which was in accordance with Higuchi equation, MTT results showed its anti-tumor inhibitory effect enhanced as time prolonging.Conclusion:PEG-PLGA-VCR-NPs was prepared by the double emulsion-solvent evaporation method with a proper size, higher encapsulation efficiency and drug loading, better stability, significant controlled release effect and stronger anti-tumour activity. |
