聚乙二醇修饰青蒿素脂质纳米粒冻干工艺优化及其表征  

Freeze-drying process optimization and characteristics of PEG modified artemisinin-loaded nanostructured lipid carriers

作　　者：赵青[1] 王芳[1] 王锐利[1] 张丽锋[1] 张淑秋[1] 

机构地区：[1]山西医科大学药学院,太原030001

出　　处：《中国药物与临床》2015年第8期1057-1059,I0002,共4页Chinese Remedies & Clinics

基　　金：国家自然科学基金(81373364)

摘　　要：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 m V,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。Objective To screen the optimal formula of cryoprotectants for PEG modified artenfisinin-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 under 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.

关 键 词：聚乙二醇类 青蒿素 工艺学 制药 

分 类 号：R943[医药卫生—药剂学]