肝靶向阿克拉霉素A固体脂质纳米粒质量考察及体内分布研究  

Study on Quality Control of Liver Targeted Aclacinomycin A Solid Lipid Nanoparticles and Its in vivo Distribution in Mice

作　　者：何林[1] 李素华[2] 吴正中[1] 蒋学华[2] 余继英[1] 

机构地区：[1]四川省人民医院药剂科,成都610072 [2]四川大学华西药学院,成都610041

出　　处：《中国药学杂志》2008年第6期431-435,共5页Chinese Pharmaceutical Journal

基　　金：四川省科技厅重点科技项目(01SY051-41)

摘　　要：目的为促进固体脂质纳米粒(SLN)的发展,提高阿克拉霉素A(ACM-A)的疗效,制备具有肝靶向的阿克拉霉素A固体脂质纳米粒(ACM-SLN)冻干针剂,并对其质量和体内组织分布进行研究。方法采用正交设计优化ACM-SLN及其冻干针剂的处方和制备工艺,并研究其形态、粒径及粒径分布、载药量,稳定性和动物体内分布。结果得到的ACM-SLN平均粒径为62 nm,平均载药量为4.41%,平均包封率为88.17%。体内分布研究结果表明,15,30和60 min时ACM-SLN冻干针剂在肝脏中的药物浓度分别为30.379,32.591和30.416 mg·L^-1而对应的ACM-A溶液剂的质量浓度分别为10.795,12.796和10.135 mg·L^-1结论得到的ACM-SLN冻干针剂基本稳定。与ACM-A溶液剂相比,ACM-SLN冻干针剂显著提高了ACM- A在靶器官肝脏中的药物水平。OBJECTIVE To investigate the quality control and its tissue distribution of the prepared liver targeted aclacinomycin A solid lipid nanoparticles（ACM-SLN）. METHODS The orthogonal design was applied to the optimization of the formula and technology of ACM-SLN. The quality characteristics of its shape, average diameter, particle distribution, drug loading, stability in vitro and tissue distribution in vivo were studied. RESULTS The average diameter of ACM-SLN was 62 nm, drug loading was 4. 47% and embedded ratio was 89. 32%. The drug concentrations of ACM-SLN in targeted liver in mice were 30. 379,32. 591 and 30. 416 mg·L^-1 in 15,30 and 60 min respectively, whereas, the corresponding concentrations of ACM-A were 10. 795, 12. 796 and 10. 135 mg·L^-1. CONCLUSION The prepared ACM-SLN was stable and there was significantly increase for the drug concentration in mice liver after iv administration of ACM-SLN comparing with ACM-A solution.

关 键 词：阿克拉霉素A 固体脂质纳米粒 靶向给药系统 质量研究 体内分布 

分 类 号：R944[医药卫生—药剂学]