R8修饰具有壳核结构的磷脂纳米粒的制备及其体外摄取研究

Study on the preparation and properties of R8 conjugated PLGA-lecithin-PEG core-shell nanoparticles in vitro

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 R8 conjugated nanoparticles of mixed lipid monolayer shell and biodegradable polymer core with PLGA and lecithin, and evaluate their physicoehemical properties and the efficiency of cellular uptake in vitro. METHODS The lipid - nanoparticles were prepared by nanopreeipitation. The appearance, particle size, Zeta potential were evaluated. The efficiency of cellular uptake on HepG2 cells in vitro was evaluated. RESULTS The particle diameter of the lipid - nanoparticles was 96.8 ± 5.5 nm with the Zeta potential of -13.50 ± 2.23 inV. The result demonstrated that the R8 -lipid -nanoparticles uptaken by HepG2 were 2. 1,3.2 times higher than that of lipid - nanoparticles and PLGA nanoparticles, respectively. CONCLUSION R8 - lipid - nanoparticles were easy to prepare and showed a significantly higher efficiency of cellular uptake than lipid - nanoparticles and PLGA nanoparticles.