中链脂肪酸-VC复合脂质体制备及初步稳定性

Preparation and Stability of Medium-chain Fatty Acid-VC Complex Liposome

以磷脂和胆固醇为膜材,脂溶性的中链脂肪酸(MCFAs)和水溶性的VC为模型药物,以脂质体的包封率和粒径为指标,分别采用薄膜法、复乳法、薄膜-高压法、复乳-高压法制备中链脂肪酸-VC复合脂质体,筛选出最佳制备方法(复乳-高压法),并通过单因素试验设计,确定复合脂质体的最优处方工艺为:总脂材质量浓度5.0g/100mL,MCFAs质量浓度10.0mg/mL,VC质量浓度3.0mg/mL,卵磷脂与胆固醇质量比为4:1,卵磷脂质量与无水乙醇体积比为1:10(g/mL),吐温与总脂材质量比为3:10,VE与卵磷脂质量比为4:100,120MPa条件下超微乳化处理2次。制备的复合脂质体MCFAs包封率达到49.01%,VC的包封率达到54.19%,平均粒径90.3nm,在4℃贮藏15d,包封率和粒径变化不大,表明脂质体低温贮藏稳定性良好。

This study was undertaken to prepare medium-chain fatty acid（MCFA）-VC complex liposome using lecithin and cholesterol as membrane materials and optimize the preparation process.Four preparation methods including thin film method,high pressure-thin film method,double emulsification method and high pressure-double emulsification method were compared in terms of entrapment efficiency and liposomal particle size.As a result,high pressure-double emulsification method was found to be the best method.One-facto-at-a-time experiments were carried out to determine the optimal preparation conditions as follows： total lipid material cocentration of 5.0 g/100 mL,MCFAs concentration of 10.0 mg/mL,VC concentration of 3.0 mg/mL,lecithin/absolute ethanol ratio of 1：10（g/mL）,mass ratio of lecithin to cholesterol of 4：1,mass ratio of Tween to total lipid material of 3：10,mass ratio of VE to lecithin of 5：1,and twice repeated ultramicroemulsification at 120 MPa,respectively. Under these optimal conditions,the entrapment efficiencies of MCFA and VC were 49.01% and 54.19%,respectively and a mean particle size of 90.3 nm was achieved.The three indexes had little change during storage at 4 ℃ for 15 days,thus indicating excellent stability at low storage temperature.