硫酸铵梯度法制备莫西沙星脂质体的工艺研究

Preparation of moxifloxacin liposomes by ammonium sulfate gradient method

目的制备具有较高包封率和载药量且体外放置稳定的莫西沙星脂质体。方法采用硫酸铵梯度法制备包载莫西沙星的脂质体,以粒径及其分布和包封率、载药量为指标对处方和工艺进行优化。结果最佳制备条件为:空白脂质体中硫酸铵质量浓度70 mg/mL、磷脂质量浓度50 mg/mL、脂质体粒径120 nm左右、透析时间5 h、载药时药脂比2∶3、孵育温度40℃、孵育时间30 min。制备得到的莫西沙星脂质体粒径为(143.00±3.98)nm,包封率为(74.56±3.21)%,载药量为(26.39±1.88)%。结论硫酸铵梯度法制备的莫西沙星脂质体包封率较高,粒径均一,室温放置稳定性良好。

Objective To prepare the moxifloxacin liposomes with high entrapment efficiency, drug loading capacity, and storage stability. Methods Ammonium sulfate gradient method was used to prepare moxifloxacin liposomes; the formulation and preparation process was optimized using the particle diameter, size distribution, entrapment efficiency, and drug loading capacity of the resultant liposomes as the evaluating indicators. Results The optimal preparation conditions included 70 mg/mL ammonium sulfate, 50 mg/mL HSPC, dialysis time of 5 h, and 120 nm in diameter for the resultant blank liposomes; the drug-lipid ratio was 2∶3, and the incubation temperature was at 40 ℃ for 30 min for drug-loading. The obtained moxifloxacin liposomes were （143.00 ± 3.98） nm in diameter, achieving high entrapment efficiency of （74.56 ± 3.21）% and drug loading capacity of （26.39 ± 1.88）%. Conclusion The moxifloxacin liposomes prepared by ammonium sulfate gradient method are with high entrapment efficiency and drug loading, capacity and are stable at room temperature.