摘要
采用乳液聚合法制备了柔红霉素聚氰基丙烯酸正丁酯毫微粒(1),并对其形态、粒径及分布、载药性、动物体内经时变化过程及骨髓靶向性进行了研究。结果表明1平均粒径为70nm,分布范围30~220nm,包封率为97.0%,载药量达55.7%(g/g);小鼠尾静脉注射相同剂量1及柔红霉素后,前者股骨内峰浓度提高到1.62倍,AUC提高到4.87倍,总靶向效率从5.17%提高至24.19%,表明1具骨髓靶向性。
The bone marrow targeting daunorubicin polybutylcyanoacrylate nanoparticles (1,DNR PBCA NP) were prepared by emulsion polymerization.The morphology,size and size distribution and drug loading of 1 lyophilization injection were studied.The results showed that the median diameter of 1 was 70 nm with the range of 30~220 nm.The association ratio was 97.0% and the drug loading was 55.7%(g/g).The tissue distribution and the bone marrow targeting characteristics of 1 and DNR injection after intravenous injection in mice were studied by HPLC.The results showed that the C max of 1 in bone marrow was increased to 1.62 fold and its AUC was increased to 4.87 fold.The overall targeting efficiency ( Te ) in the bone marrow was increased from 5.17% to 24.19%.\;
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2000年第2期57-61,共5页
Chinese Journal of Pharmaceuticals
关键词
柔红霉素
毫微粒
DNR-PBCA-NP
骨髓靶向性
bone marrow targeting drug delivery system
daunorubicin
polybutylcyanoacrylate nanoparticles
surface modification