聚乙二醇修饰青蒿素脂质纳米粒冻干工艺优化及其表征

摘要

Objective To screen the optimal formula of cryoprotectants for PEG modified artemisinin-loaded nanostructured lipid carriers (PEG-ART-NLC) and to investigate its freeze-drying process and characteristics. Methods Different cryoprotectants were used to prepare PEG-ART-NLC freeze-drying powder. The cryoprotectants were optimized based on the appearance, redispersibility, redissolved appearance, particle size and Zeta potential of the PEG-ART-NLC freeze-drying powder. The quality changes of PEG-ART-NLC before and after freeze-drying were compared. Results The mixture of 4%mannitol and 4%sucrose showed good protective effect and redispersibility. The PEG-ART-NLC par-ticle size was increased by 14.0 nm, and the Zeta potential absolute value and encapsulation efficiency were decreased by 8.8 mV and 14.5%, respectively. The morphology of the PEG-ART-NLC freeze-drying powder was round or oval un-der electron microscope before and after freeze-drying, without significant differences. Conclusion A stable kind of PEG-ART-NLC freeze-drying powder can be prepared by the optimal cryoprotectants of 4%mannitol and 4%sucrose.%目的：筛选聚乙二醇（PEG）修饰青蒿素脂质纳米粒（PEG-ART-NLC）最优冻干保护剂处方，研究其冷冻干燥工艺及质量表征。方法制备含不同冻干保护剂的PEG-ART-NLC冻干粉，以外观、再分散性、复溶后外观、粒径、Zeta电位为指标，优化保护剂处方，并对比冻干前后脂质纳米粒质量变化。结果4％甘露醇和4％蔗糖具良好的保护作用和再分散性，冻干后纳米粒粒径增大14.0 nm，Zeta电位绝对值降低8.8 mV，包封率降低14.5％，电镜下冻干前后纳米粒形态均为圆形或椭圆形，无明显差异。结论4％甘露醇和4％蔗糖为最优保护剂处方，可用于制备稳定的PEG-ART-NLC冻干粉。