【摘要】 目的:制备马钱子总生物碱隐形脂质体并与普通脂质体比较急性毒性。方法:采用酸性染料法测定马钱子总生物碱的含量。采用氨性氯仿法从制马钱子中提取了马钱子总生物碱并测定了纯度。以士的宁为模型药物,考察马钱子总生物碱隐形脂质体的制备工艺。采用硫酸铵梯度法制备了马钱子总生物碱隐形脂质体及普通脂质体,比较了两者的包封率、粒径等药剂学性质以及急性毒性。结果:采用优化后的处方与工艺,士的宁隐形脂质体的包封率为90.64%,产率为98.82%,并应用于马钱子总生物碱隐形脂质体的制备。马钱子总生物碱隐形脂质体和普通脂质体的包封率分别为80.97%和73.01%,粒径分别为106.5 nm和163.4 nm。马钱子总生物碱溶液、普通脂质体及隐形脂质体的LD50分别为1.85、2.56和3.42 mg/kg。结论:士的宁隐形脂质体的制备工艺可用于马钱子总生物碱隐形脂质体制备。与普通脂质体相比,隐形脂质体作为马钱子总生物碱的载体性质更加理想。更多还原

【Abstract】 AIM: To prepare stealth liposomes containing total alkaloids from seeds of Strychnou nux-vomica L.and compare the acute toxicity with corresponding conventional liposomes. METHODS: The content of total alkaloids in the samples was determined by the acidic dyecolorimetry,which was performed with brucine as the reference substance.The total alkaloids and the purity were determined.The optimal technique of strychnine stealth liposome was used to prepare stealth liposome containing total alkaloids.Stealth liposomes and conventional liposomes containing the total alkaloids were both prepared by ammonium sulfate transmembrane gradients.The encapsulation efficiency,particle size and acute toxicity were compared between stealth liposomes and conventional liposomes. RESULTS: By the use of optimized prescription and technique,the entrapment efficiency and yield efficiency of strychnine stealth liposome were 90.64% and 98.82%,respectively.The encapsulation efficiency of stealth liposomes and conventional liposomes were 80.97% and 73.01%,respectively.The mean particle sizes were 106.5nm and 163.4nm,respectively.The LD₅₀ of solution,conventional liposomes and stealth liposomes were 1.85,2.56 and 3.42 mg/kg,respectively. CONCLUSION: The optimized preparation method of strychnine stealth liposome can be used to prepare corresponding stealth liposome containing total alkaloids from seeds of Strychnou nux-vomica L.As the drug delivery system,the characteristics of stealth liposomes are more satisfactory than the corresponding conventional liposomes.更多还原