目的 制备四环素介导的聚乙二醇-聚(乳酸-羟基乙酸)载阿托伐他汀(TC-PEG-PLGA/ATO)胶束，并且考察载药胶束的理化性质及其体外靶向性。方法 通过脱水反应合成具有两亲性的TC-PEG-PLGA嫁接物并对其进行结构确证，利用透析法实现对水难溶性药物阿托伐他汀的负载，采用透射电镜观察载药胶束的形态，激光粒度分析仪测定载药胶束的粒径和Zeta 电位，HPLC测定胶束载药量和包封率，透析法考察载药胶束的体外释放行为。对TC-PEG-PLGA嫁接物胶束的体外细胞毒性(MTT法)和羟基磷灰石靶向能力进行评价。结果 本实验成功制备了TC-PEG-PLGA/ATO载药胶束，其平均粒径为(47.2±4.7)nm，电位值为(-14.25±0.31) mV，包封率为(98.2±1.51)%，载药量为(8.71±0.23)%，体外释放研究表明，48 h 时药物的累计释放率接近70%，具有明显的缓释作用。MTT结果表明，空白胶束在100~500 μg·mL^-1内生物相容性良好。骨靶向TC-PEG-PLGA胶束(87.94%)的羟基磷灰石亲和能力相比于比PEG-PLGA胶束(18.59%)提高了4.73倍。结论 本实验成功构建TC-PEG-PLGA/ATO载药胶束，其粒径小，稳定性好，可显著提高ATO在水相中的浓度，在体外具有良好的缓释效果、安全性及对羟基磷灰石的亲和力。

OBJECTIVE To prepare atorvastatin-loaded tetracycline-PEG-PLGA(TC-PEG-PLGA/ATO) polymeric micelles, and investigate its pharmaceutical characteristics and targeting function in vitro. METHODS The amphiphilic TC-PEG-PLGA conjugate was synthesized via an esterification reaction and identified by the ¹H-NMR. Water insoluble atorvastatin was loaded on TC-PEG-PLGA conjugate micelles via dialysis method. The morphology of TC-PEG-PLGA/ATO micelles was observed under transmission electron microscope. The particle size distribution and Zeta potential of TC-PEG-PLGA/ATO micelles were determined by dynamic light scattering method. The drug loading and encapsulation efficiency were measured by HPLC, and in vitro release behavior was investigated via dialysis method. In vitro cytotoxicity was assessed via MTT assay, and bone-targeting activity was investigated via binding to the hydroxyapatite powder. RESULTS TC-PEG-PLGA/ATO micelle was prepared successfully, and its particle size and Zeta potential were (47.2±4.7) nm and (-14.25±0.31) mV. The encapsulation efficiency and drug loading rate were(98.2±1.51)% and (8.71±0.23)%, respectively. Moreover, the accumulative release of ATO in vitro was about 70% in 48 h, which indicated that the drug was released slowly from the micelles. In vitro cell evaluation showed that TC-PEG-PLGA conjugate micelles were great biocompatibility with MC3T3-E1 cells within the concentration range of 100-500 μg·mL^-1. In vitro targeting performance indicated that the proportion of the TC-PLGA NPs bound to Hap(87.94%) was greater than the bound proportion of PLGA NPs(18.59%). CONCLUSION The TC-PEG-PLGA/ATO micelles exhibit small partical size and good stability, and significantly increased ATO content in aqueous solution. TC-PEG-PLGA/ATO micelles have good delayed release behavior, safety and binding efficacy to the hydroxyapatite powder.