阿霉素高聚物胶束的制备及其体外抗肿瘤活性研究  

Preparation and Research on the Anti-Tumor Activity of Doxorubicin Loaded High Polymer Micelles

作　　者：许向阳[1] 周建平[1] 李玲[1] 施丹霞 卢是玥 杨洁[2] 霍美蓉[1] 

机构地区：[1]中国药科大学药剂学教研室,南京210009 [2]江苏先声药物研究有限公司,南京210042

出　　处：《中国药学杂志》2008年第7期514-518,共5页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(30472105)

摘　　要：目的制备阿霉素高聚物胶束并研究其体外抗肿瘤活性。方法以N-正辛基-N′-琥珀酰基壳聚糖为载体,采用透析法制备阿霉素胶束,并测定其载药量、包封率、形态、粒径、表面电位(Zeta电位),及其对K562,HepG2肿瘤细胞的细胞毒作用。结果阿霉素高聚物胶束载药量为35.8%,包封率为75.3%,粒径控制在100～200nm,药物体外释放较缓慢,对K562肿瘤细胞及HepG2细胞的细胞毒作用优于阿霉素。结论N-正辛基-N′-琥珀酰基壳聚糖不仅是阿霉素的优良载体,且可提高抗K562,HepG2肿瘤细胞的活性。OBJECTIVE To prepare doxorubicin loaded N-octyl-N＇-succinyl chitosan micelles and study the in vitro anti-tumor activity.METHODS The doxorubicin loaded N-octyl-N＇-succinyl chitosan micelles were prepared by dialysis and were characterized by drug loading content,entrapment efficiency,morphology,particle size,and Zeta potential.They were incubated with K562 cells and HepG2 cells to assess the inhibition ability of doxorubicin loaded N-octyl-N＇-succinyl chitosan.RESULTS Doxorubicin loaded N-octyl-N＇-succinyl chitosan micelles were prepared with loading content of 35.8% and entrapment efficiency of 75.3%,small size range of 100～200 nm,and slow release in vitro.The inhibition ability against K562 or HepG2 was stronger than doxorubicin alone.CONCLUSION N-octyl-N＇-succinyl chitosan used as tumor-targeting carrier of doxorubicin exhibited more cytotoxic activity against K562 or HepG2 than doxorubicin alone.

关 键 词：N-正辛基-N′-琥珀酰基壳聚糖 胶束 体外抗肿瘤活性 

分 类 号：R944[医药卫生—药剂学]