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目的:研究PEG化呋喃二烯固体脂质纳米粒(PEG-FDE-SLN)的制备方法,并考察其理化性质及细胞摄取性能。方法:实验采用乳化蒸发-低温固化法制备PEG-FDE-SLN,以粒径、Zeta电位、多分散系数、包封率为评价指标,通过单因素考察选择制备PEG-FDE-SLN的最佳处方。以小鼠腹腔巨噬细胞(MPM)为模型做体外细胞摄取实验。结果:制备PEG-FDE-SLN的最佳处方为固态脂质单硬脂酸甘油酯100 mg,液态脂质中碳链三酰甘油40 mg,乳化剂蛋黄卵磷脂13 mg,聚乙二醇硬脂酸酯150 mg,制备的样品粒径为(272.9±2.4)nm,多分散系数为(0.193±0.022),Zeta电位为(-19.82±0.52)mV。包封率为(90.0±1.0)%。体外细胞摄取实验证明,MPM对FDE-SLN的摄取随着聚乙二醇硬脂酸酯的加入以及PEG相对分子质量的增加而逐渐减小,以PEG5000-FDE-SLN摄取最少为(8.4±0.4)%。结论:本实验制备的PEG-FDE-SLN,能够改善巨噬细胞对FDE-SLN的摄取作用,PEG链长度影响MPM对FDE-SLN的摄取作用,PEG链越长MPM摄取越少。
Objective: To study the preparation method of PEG-FDE-SLN and study its physicochemical properties and cell uptake. METHODS: PEG-FDE-SLN was prepared by emulsion evaporation-low temperature curing method. The optimum prescription of PEG-FDE-SLN was selected by single factor test with particle size, Zeta potential, polydispersity and entrapment efficiency . Mouse peritoneal macrophages (MPM) as a model in vitro cell uptake experiments. Results: The best prescription for preparing PEG-FDE-SLN was solid lipid glyceryl monostearate 100 mg, liquid lipid medium chain triglyceride 40 mg, emulsifier egg yolk lecithin 13 mg, polyethylene glycol hard The diameter of the prepared sample was (272.9 ± 2.4) nm. The polydispersity index was (0.193 ± 0.022) and the zeta potential was (-19.82 ± 0.52) mV. The encapsulation efficiency was (90.0 ± 1.0)%. In vitro cellular uptake experiments demonstrated that uptake of FDE-SLN by MPM decreased gradually with the addition of polyethylene glycol stearate and the increase of molecular weight of PEG, and the uptake by PEG5000-FDE-SLN was at least (8.4 ± 0.4 )%. Conclusion: PEG-FDE-SLN prepared in this study can improve the uptake of FDE-SLN by macrophages. PEG chain length affects the uptake of FDE-SLN by MPM.