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目的制备棓丙酯脂质体,并对其进行理化性质的表征和释放度的评价。方法采用薄膜分散法制备棓丙酯脂质体,超滤离心法测定脂质体的包封率,正交设计优化处方,并对其包封率、粒径、Zeta电位、形态及体外释放行为进行综合评价。结果正交设计优化最终处方为磷脂浓度5 mg.mL-1、药脂比1∶5、磷脂胆固醇比5∶1、水化介质离子强度20 mmol.mL-1,所得脂质体包封率为89.6%、粒径为181.3 nm、Zeta电位为-21.8 mV、4 h体外释放达到80%。结论制备的棓丙酯脂质体包封率高,粒径小而均一,体外释放完全。
OBJECTIVE: To prepare the promethazine liposomes, and to evaluate its physicochemical properties and release. Methods The prodrug liposomes were prepared by membrane dispersion method. The entrapment efficiency and orthogonal design were optimized by ultrafiltration centrifugation. The encapsulation efficiency, particle size, zeta potential, morphology and in vitro release Conduct a comprehensive evaluation. Results Orthogonal design optimization of the final prescription for the phospholipid concentration of 5 mg.mL-1, lipid-lipid ratio of 1: 5, phospholipid cholesterol ratio of 5: 1, ionic strength of hydration medium 20 mmol.mL-1, the resulting liposome entrapment efficiency Was 89.6% with a particle size of 181.3 nm and a zeta potential of -21.8 mV, reaching 80% in vitro in 4 h. Conclusion The prepared propidium ester liposomes have high encapsulation efficiency, small and uniform particle size and complete release in vitro.