阿仑膦酸修饰的水凝胶负载柚皮素骨靶向系统构建及其增强成骨分化作用

目的 中药黄酮类单体存在水溶性较差、生物利用度低等特点，低效率全身给药的方式限制其在治疗骨疾患的应用，本研究旨在改善黄酮类单体治疗骨质疏松局限现状。方法 本研究制备了阿仑膦酸修饰的水凝胶负载中药骨碎补活性黄酮单体柚皮素的凝胶载药系统，通过活体荧光技术验证其骨靶向性能，并进一步采用PCR、WB等技术探究了该凝胶载药系统的促进成骨分化效用。结果 制备的凝胶载药系统促进成骨且稳定性好，释药部位集中于大鼠骨组织，干预成骨细胞MC3T3-E1细胞后，其成骨因子及相关蛋白表达明显增强。结论 阿仑膦酸修饰的水凝负载柚皮素可实现骨靶向大鼠骨组织，且能有效促进成骨分化，从而可潜在实现治疗骨质疏松。

Construction of Alen modified hydrogel loaded naringenin bone targeting system and verification of its effect on enhancing osteogenic differentiation

Objective Traditional Chinese medicine flavonoid monomers have the characteristics of poor water solubility and low bioavailability. The low efficiency of systemic administration limits its application in the treatment of bone diseases. In order to improve the limited status of flavonoid monomers in the treatment of osteoporosis. Methods In this study, the gel delivery system of alendronate modified hydrogel loaded with naringenin, the active flavonoid monomer of Chinese traditional medicine, was prepared. Its bone targeting performance was verified by in vivo fluorescence technology, and the effect of the gel delivery system on promoting osteogenic differentiation was further explored by PCR and WB techniques. Results The prepared gel drug delivery system was successfully prepared and had good stability. The drug release site was concentrated in rat bone tissue. After intervention with osteoblast MC3T3-E1 cells, the expression of osteogenic factors and related proteins was significantly enhanced.Conclusion Alendronic acid modified hydrogel loaded naringenin can achieve bone targeting in rat bone tissue, and can effectively promote osteogenic differentiation, which can potentially achieve the treatment of osteoporosis.