The preparation and acute toxicity of stealth liposomes containing total alkaloids from seeds of Strychnos nux-vomica L / 中成药

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 LD_(50) 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.