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目的采用磷脂和聚乳酸羟基乙酸共聚物(PLGA)制备细胞穿膜肽R8介导的具有壳核结构的磷脂纳米粒,筛选处方并考察其理化性质和体外细胞摄取效率。方法采用一步沉淀法制备具有壳核结构的磷脂纳米粒,考察其形态、粒径及电位,并通过HepG2细胞与PLGA纳米粒比较摄取效率。结果所制备的R8修饰磷脂纳米粒在电镜下观察其外观为球形,平均粒径为96.8±5.5 nm,Zeta电位为-13.50±2.23 mV。体外细胞摄取实验表明:HepG2细胞对经R8修饰的磷脂纳米粒的摄取效率分别是无R8修饰的磷脂纳米粒和PLGA纳米粒的2.1倍和3.2倍。结论该磷脂纳米粒制备方法简单,与无R8修饰磷脂纳米粒和PLGA纳米粒相比,经R8和磷脂修饰的纳米粒可显著提高细胞摄取效率。
OBJECTIVE To prepare phospholipid nanoparticles with a putamen structure mediated by phospholipids and poly (lactic-co-glycolic acid) (PLGA) and to investigate the physicochemical properties and in vitro cell uptake efficiency. Methods The phospholipid nanoparticles with putamen structure were prepared by one-step precipitation method. Morphology, particle size and potential were investigated. The uptake efficiency of HepG2 cells was compared with that of PLGA nanoparticles. Results The R8-modified phospholipid nanoparticles prepared in this study showed a spherical shape with a mean diameter of 96.8 ± 5.5 nm and a Zeta potential of -13.50 ± 2.23 mV under electron microscopy. In vitro cell uptake experiments showed that the uptake efficiency of HepG2 cells by R8 modified phospholipid nanoparticles were 2.1 times and 3.2 times that of non-R8 modified phospholipid nanoparticles and PLGA nanoparticles, respectively. Conclusion The preparation method of phospholipid nanoparticles is simple. Compared with non-R8 modified phospholipid nanoparticles and PLGA nanoparticles, nanoparticles modified by R8 and phospholipid can significantly improve the cell uptake efficiency.