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目的制备拟低密度脂蛋白纳米脂质载体(recombinant low density lipoprotein,rLDL)的脂质核心部分并考察其制剂学和生物学性质。方法采用乳化-超声法制备脂质核心,以粒径大小为指标优化制备工艺及处方。在获得制剂学最优处方基础上以细胞摄取率为指标,使用星点设计法优化生物学处方,并比较两种处方的制剂学性质。结果所制备的脂质核心溶液每毫升中含胆固醇0.25 mg、胆固醇油酸酯6.00 mg、磷脂4.50 mg、三油酸甘油酯1.50 mg为较优的制剂学处方,其细胞摄取率约为21.22%;每毫升制剂中含胆固醇0.32 mg、胆固醇油酸酯7.80 mg、磷脂3.86 mg、三油酸甘油酯1.52 mg为较优的生物学处方,摄取率约为34.17%。制得的两种脂质核心粒径分别为(180±23)nm和(200±27)nm,4℃静置15 d外观均无明显变化。结论纳米脂质核心生物学最优处方制备工艺简单、粒径小、稳定性好、细胞摄取率高。
Objective To prepare the lipid core of recombinant low density lipoprotein (rLDL) and investigate the preparation and biological properties. Methods The lipid core was prepared by emulsification - ultrasonic method, and the preparation process and prescription were optimized by the size of particle. On the basis of obtaining the optimal preparation prescription, taking the cell uptake rate as an index, the biological prescription was optimized by using the star design method, and the formulation properties of the two prescriptions were compared. Results The prepared lipid core solution contained 0.25 mg of cholesterol, 6.00 mg of cholesterol oleate, 4.50 mg of phospholipid and 1.50 mg of glyceryl trioleate per ml, which was the optimal preparation formulation with a cell uptake rate of about 21.22% ; Per ml of preparation containing cholesterol 0.32 mg, cholesterol oleate 7.80 mg, phospholipid 3.86 mg, triolein 1.52 mg for better biological prescription, the uptake rate of about 34.17%. The diameters of the two lipid cores obtained were (180 ± 23) nm and (200 ± 27) nm, respectively. There was no significant change in the appearance of the two lipids after standing at 4 ° C for 15 days. Conclusion The optimum preparation method of nanolipid core biology is simple, the particle size is small, the stability is good, and the cell uptake rate is high.