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目的制备二甲双胍阿霉素脂质体并对其制备工艺进行优化。方法以二甲双胍阿霉素脂质体的包封率为评价指标,对其处方和制备工艺进行筛选和优化。分别考察了磷脂与胆固醇的比例、水化介质中阴离子的种类、水化介质的浓度、水化介质的pH值、载药温度、载药时间对二甲双胍阿霉素脂质体包封率的影响。结果最终优化的处方为m(hydrogenated soybean phosphatidylcho-line,HSPC)∶m(cholesterol,CH)∶m(polyethylene glycol 2000-cholesteryl hemisuccinate,mPEG2000-CHEMS)=3.0∶1.0∶1.0,以pH为7.00的300 mmol.L-1的枸橼酸二甲双胍为水化介质,60℃载药60 min,所制备的脂质体包封率可达98.7%。结论以枸橼酸二甲双胍离子梯度法制备的阿霉素脂质体包封率高,方法可行。
Objective To prepare metformin doxorubicin liposomes and optimize its preparation process. Methods The entrapment efficiency of doxorubicin liposomes as evaluation index, the prescription and preparation process were screened and optimized. The effects of the ratio of phospholipid to cholesterol, the type of anions in hydration medium, the concentration of hydration medium, the pH value of hydration medium, the drug loading temperature and drug loading time on the entrapment efficiency of doxorubicin . Results The final optimized formulation was m (polyethylene glycol 2000-cholesteryl hemisuccinate: mPEG2000-CHEMS) = 3.0: 1.0: 1.0, pH was 300 mmol.L-1 citrate citrate as a hydration medium, 60 ° C for 60 min, the prepared liposome encapsulation efficiency up to 98.7%. Conclusion The doxorubicin liposome prepared by the metformin citrate citrate gradient has high encapsulation efficiency.