骨髓靶向柔红霉素毫微粒的研究

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平均微粒径为７０ｎｍ，分布范围３０－２２０ｎｍ，包封率为９７．０％，载药一达５５．７％；小鼠胸脉注射相同剂量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％提高到２４．１９％，表明１具骨髓靶向性。

Study on Bone Marrow Targeting Daunorubicin Polybutylcyanoacrylate Nanoparticles

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%.