Bone pain is the primary problem for patients with osteoporosis. Ketoprofen is clinically used to treat osteoporotic pain, while long-term oral administration of ketoprofen can cause some side effects. In addition, osteoporosis is also accompanied by bone mass loss and inflammation. In this study, we designed a multifunctional drug (Ket@Mg-MOF-74) adopted Mg-MOF-74 to load ketoprofen to treat osteoporotic pain, bone loss and inflammation comprehensively. Mg-MOF-74 was prepared, and the physicochemical characterization proved that it had excellent physical and chemical stability. Ket@Mg-MOF-74 was synthesized by post-synthetic modification method and a high loading rate of ketoprofen was confirmed. Drug release and ion release experiments indicated Ket@Mg-MOF-74 had a good controlled release of ketoprofen and Mg in solution. Cell experiments in vitro proved the compound drug could significantly reduce the expression of pain-related genes of cyclooxygenase 2 (COX2), obviously up-regulated the expression of osteogenic cytokines and remarkably down-regulated the secretion of pro-inflammatory factors. Therefore, Ket@Mg-MOF-74 is believed a promising painkiller for osteoporotic bone pain, with the function of anti-inflammatory and promoting bone formation.

骨痛是骨质疏松症患者的首要问题。酮洛芬临床上用于治疗骨质疏松性疼痛，而长期口服酮洛芬会引起一些副作用。此外，骨质疏松症还伴随着骨量减少和炎症。在本研究中，我们设计了一种多功能药物（Ket@Mg-MOF-74），采用Mg-MOF-74负载酮洛芬，综合治疗骨质疏松性疼痛、骨质流失和炎症。制备了Mg-MOF-74，理化表征证明其具有优异的理化稳定性。Ket@Mg-MOF-74 是通过合成后修饰的方法合成的，并证实了酮洛芬的高负载率。药物释放和离子释放实验表明，Ket@Mg-MOF-74 在溶液中对酮洛芬和 Mg 具有良好的控制释放。体外细胞实验证明，复方药物可显着降低疼痛相关基因环加氧酶2（COX2）的表达，明显上调成骨细胞因子的表达，显着下调促炎因子的分泌。因此，Ket@Mg-MOF-74被认为是一种很有前途的骨质疏松性骨痛止痛药，具有抗炎和促进骨形成的作用。