果胶-壳聚糖多层修饰脂质体的制备及配方优化
Preparation of pectin-chitosan layer by layer modified liposomes and the formula optimization
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摘要: 本研究利用壳聚糖、果胶对常规脂质体进行先后修饰构建果胶-壳聚糖多层修饰脂质体(pectin-chitosan coated liposomes,Pe-Ch-Liposomes),以番茄红素为模型药物,系统研究了主要因素对多层修饰脂质体包封率和浊度的影响,并以包封率为指标优化配方。结果表明果胶溶液与壳聚糖溶液的体积及浓度配比均对多层修饰脂质的包封率及浊度有一定的影响,且多层修饰过程可降低由卵磷脂与胆固醇质量比引起的包封率及浊度的差异。正交实验结合单因素分析确定最佳配方为果胶壳聚糖体积比为2∶1,果胶-壳聚糖总浓度为0.2%∶0.2%,卵磷脂与胆固醇质量比为5∶1,番茄红素添加量为2.5 mg。在此条件下制备的多层修饰脂质体的包封率(97.8%)显著高于常规脂质体的包封率(85.4%);粒度分布较为集中,平均粒径为1870.4 nm,多分散系数为0.231。Abstract: In this research pectin-chitosan layer by layer modified liposomes were successfully prepared. The effects of main factors on the encapsulation efficiency and turbidity were evaluated,and optimal formula was obtained by orthogonal experiments using encapsulation efficiency as the main index.The results indicated that the volume ratio and concentration ratio of pectin solution to chitosan solution had significant effects on the encapsulation efficiency and turbidity of pectin-chitosan layer by layer modified liposomes. The process of modification could diminish the properties differences affected by the mass ratio of lecithin to cholesterol. The optimal formula was the volume ratio of pectin solution to chitosan solution 2 ∶ 1,concentrations of pectin solution and chitosan solution 0.2% ∶ 0.2%,the mass ratio of lecithin to cholesterol 5∶ 1,addition amount of lycopene 2.5 mg.The encapsulation efficiency of the optimized pectin-chitosan modified liposomes was significantly higher than that of conventional liposomes,which was 97.8% and 85.4% for them,respectively,the particle size distribution of the obtained pectin-chitosan modified liposomes was narrow with the mean particle size of 1870.4 nm and polydispersity index of 0.231.