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目的制备白蛋白包覆纳米脂质载体,考察其理化性质及生物学性质。方法采用乳化超声-低温固化法制备白蛋白包覆纳米脂质载体。在前期单因素考察结果的基础上,利用三因素三水平Box-Behnken效应面法筛选最佳处方,并对其外观形态、粒径分布、zeta电位及体外释放等理化性质进行考察。通过细胞摄取实验考察载体在不同时间及不同质量浓度条件下,在MCF-7细胞中的摄取情况。结果最优处方为固液脂质质量比为2.01,大豆卵磷脂与硬脂酸聚氧乙烯(40)酯质量比为8.55,牛血清白蛋白的质量浓度为2.13 g·L-1。包载香豆素-6的载体外观多呈圆形,粒径分布均匀,平均粒径为(209.31±5.20)nm,zeta电位为-(46.5±20)μV,48 h累计释放49.36%。MCF-7细胞对40μg·L-1的载体4 h的摄取量达到饱和。结论 Box-Behnken效应面法可用于预测和优化白蛋白包覆纳米脂质载体的处方;载体体外释放符合缓释制剂的要求;MCF-7细胞对载体的摄取具有时间质量浓度依赖性。
OBJECTIVE: To prepare albumin-coated nano-lipid carriers and study their physico-chemical properties and biological properties. Methods The albumin-coated nano-lipid carrier was prepared by emulsification-ultrasound-low temperature curing method. On the basis of the previous single-factor investigation, the best prescription was screened by the three-factor and three-level Box-Behnken effect surface method. The physical and chemical properties such as appearance morphology, particle size distribution, zeta potential and in vitro release were investigated. The uptake of MCF-7 cells in different time and different mass concentration conditions was investigated by cell uptake assay. Results The optimal formulation was solid-liquid lipid mass ratio 2.01, mass ratio of soybean lecithin to polyoxyethylene 40 stearate 8.55, and bovine serum albumin 2.13 g · L -1. The carrier containing coumarin-6 was mostly round in shape with average particle size of (209.31 ± 5.20) nm and zeta potential of - (46.5 ± 20) μV, with a cumulative release of 49.36% after 48 h. The uptake of MCF-7 cells into the 40μg · L-1 vector for 4 h reached saturation. Conclusion The Box-Behnken effect surface method can be used to predict and optimize the prescription of albumin-coated nano-lipid carrier. The in vitro release of the carrier meets the requirements of sustained-release preparations. The uptake of the carrier by MCF-7 cells has a time-dependent mass concentration dependence.