Abstract: Objective: To study the effect of Nobiletin (NOB)-nano-poly(ethylene glycol)-block-poly(e-caprolactone) (mPEG-PCL) micelles on osteoporosis osteoclasts. Methods: The drug-loaded micelles（NOB）was obtained by dialysis bag method. The particle size was determined by Malvern particle size analyzer. The morphology of the nanoparticles was investigated by transmission electron microscopy and the in vitro release behavior of the nanoparticles was investigated.The biocompatibility of blank micelles and drug-loaded micelles on macrophages and the expression of osteoclast-related genes were examined. Results: The encapsulation efficiency and loading efficiency of the drug-loaded nanoparticles was 76.34 ± 3.25% and 7.60±0.48%, and the particle size was 124 nm. The transmission electron microscopy showed that the nanoparticles were uniform in particle size and distributed in a spherical shape. The cumulative release was 65% at 12 h. The TRAP+ osteoclasts numbers and gene expression of TRAP were significantly decreased (P < 0.05) in NOB-PEG-PCL group. Conclusion: The results show that the NOB-PEG-PCL nanoparticles obviously reduce the number of osteoclasts which can be further applied to periodontal bone tissue engineering.

Key words: Nobiletin, nanoparticles, osteolasts

摘要： 目的：研究载川陈皮素(Nobiletin，NOB) 纳米粒（Nanoparticles, NPs）对破骨细胞的作用。方法：通过透析法制备载川陈皮素纳米胶束（NOB-poly(ethylene glycol)-block-poly(e-caprolactone micelles，NOB-PEG-PCL)，以包封率和粒径作为评价指标。采用Malvern粒度仪测定纳米粒的粒径分布，透射电镜考察其形态，并考察纳米粒的体外释放行为。检测空白胶束和载药胶束对破骨细胞前体巨噬细胞的生物相容性，以及对破骨细胞相关基因的表达影响。结果：川陈皮素载药纳米粒的包封率为76.34 ± 3.25%，载药量为7.60±0.48%，粒径为124nm，透射电镜显示纳米粒粒径均一，成球状分布，12h累积释放为65%，实验组NOB-PEG-PCL TRAP细胞阳性细胞数以及TRAP基因显著减少（P <0.05。结论：实验表明载川陈皮素纳米粒能明显地减少骨质疏松下破骨细胞数量，可进一步应用于牙槽骨骨组织工程。

关键词: 川陈皮素, 纳米粒, 破骨细胞