冰片-葛根素脂质体的制备及其脑靶向性研究Δ

摘要

OBJECTIVE:To prepare borneol-puerarin liposomes,and to investigate its brain-targeting. METHODS:Film dis-persion ultrasonic method was used to prepare borneol-puerarin liposomes. The morphology of liposomes was observed by TEM;the particle size and Zeta potential were measured by laser particle size analyzer;the entrapment efficiency were measured by sepha-dex gel filtration method. Compared with Puerarin injection,brain-targeting of borneol-puerarin liposomes and puerarin liposomes via intravenous injection of mice tail was studied with relative intake rate and peak concentration ratio. RESULTS:Borneol-puerarin liposomes were spherical or quasi-circular;its mean particle size,polydispersity index and Zeta potential were 226 nm,0.263 and-21.3 mV respectively. The entrapment efficiency were(65.32±2.13)%. Compared with Puerarin injection,relative intake rate of puerarin liposome and borneol-puerarin liposome were 1.68 and 2.58,and peak concentration ratio were 1.15 and 1.42. CONCLU-SIONS:Brain-targeted borneol-puerarin liposomes are prepared successfully.%目的：制备冰片-葛根素脂质体，并考察其脑靶向性。方法：采用薄膜分散超声法制备冰片-葛根素脂质体，透射电子显微镜观察脂质体形态，激光粒度仪测定其粒径和Zeta电位，葡聚糖凝胶过滤法测定包封率。以葛根素注射液为参照，以相对摄取率和峰浓度比考察小鼠尾iv葛根素脂质体、冰片-葛根素脂质体的脑靶向性。结果：制备的冰片-葛根素脂质体呈圆形或类圆形，平均粒径为226 nm，多分散指数为0.263，Zeta电位为－21.3 mV，包封率为（65.32±2.13）％。以葛根素注射液为参照，葛根素脂质体和冰片-葛根素脂质体的相对摄取率分别为1.68、2.58，峰浓度比分别为1.15、1.42。结论：成功制得具有较好脑靶向性的冰片-葛根素脂质体。