奥沙利铂脂质体的制备工艺研究

Research on the Preparation of Oxaliplatin Liposome

对奥沙利铂脂质体的最优处方和最佳制备工艺进行研究,以包封率为指标,通过薄膜蒸发法、乙醇注入法、乙醚注入法、逆向蒸发法4种不同的方法制备奥沙利铂脂质体;对奥沙利铂脂质体制备过程中奥沙利铂用量、胆固醇-卵磷脂比例、水化温度进行单因素考察。结果表明,乙醇注入法为制备奥沙利铂脂质体最佳方法,最佳制备工艺为奥沙利铂用量5 mg、胆固醇-卵磷脂比例1∶5、水化温度55℃。以优化工艺制得的脂质体形态均匀,平均粒径245.6 nm,包封率为69.10%。以优化工艺制得的奥沙利铂脂质体粒径小、包封率较高,可作为奥沙利铂脂质体的常规制备方法。

To optimize the prescription and preparation of oxaliplatin liposome. The liposome were prepared by the following methods： thin film vesicles method, ethanol injection method, diethyl ether injection method, reverse-phase evaporation vesicles method; the best prescription and preparation of oxaliplatin liposome was investigated by single factor. Experimental factors： the dosage of the oxaliplatin, the ratio of lecithin and cholesterol, and the temperature of the aqueous bath. According to the entrapment efficiency of the oxaliplatin liposome, ethanol injection method was the best method for the preparation of oxaliplatin liposome. The best experimental factors： lecithin：cholesterol was 1：5, the dosage of the oxaliplatin was 5 mg, the temperature of the aqueous bath was 55 12. The liposome had homogeneous shape with the average particle size at 245.6 nm and the envelope efficiency of oxaliplatin liposomes at 69.10 %. The experiment showed that oxaiiplatin liposome prepared by the optimized prescription and preparation had low particle size and high envelope efficiency. Therefore, it was warranted for wide use to prepare oxaliplatin liposome.