目的 制备雷公藤甲素叶酸靶向纳米胶束（TP@PCL-PEG-FA），并研究其体外抗炎效果。方法 采用薄膜水化法制备TP@PCL-PEG-FA胶束，对粒径和电位进行表征，观察其形态特征，采用超滤法测定包封率和载药量，同时考察药物的体外释放。观察胶束的摄取效率，考察体外抗炎作用。结果 TP@PCL-PEG-FA胶束的平均粒径为（34.1±5.1） nm，Zeta电位为（-10.1±2.2） mV，呈类球形，粒径分布均一。包封率为（85.7±5.8）%，载药量为（1.8±0.5）%。TP@PCL-PEG-FA胶束均能够相对缓慢释放药物，具有缓释效果。与普通非靶向PCL-PEG胶束相比，PCL-PEG-FA胶束在脂多糖刺激的RAW 264.7细胞中的摄取效率明显提高，TP@PCL-PEG-FA胶束有更强的体外抗炎效率。结论 制备了雷公藤甲素的叶酸靶向的TP@PCL-PEG-FA胶束，具有更好的体外靶向抗炎作用，为雷公藤甲素的纳米递药系统提供了一种新策略和新思路。

Objective To prepare triptolide-loaded folic acid-modified micelles (TP@PCL-PEG-FA), and study the in vitro anti-inflammatory effect. Methods TP@PCL-PEG-FA micelles were prepared with thin-film hydration method. The size distribution, Zeta potential, and morphology of TP@PCL-PEG-FA micelles were characterized. The encapsulation efficiency (EE) and drug loading capacity (DL) of micelles were determined by ultrafiltration method, and the in vitro release of triptolide was also studied. The cellular uptake efficiency and in vitro anti-inflammatory effect of micelles were evaluated. Results The average size of TP@PCL-PEG-FA micelles was (34.1 ± 5.1) nm, the Zeta potential was (-10.1 ± 2.2) mV. The micelles were spherical shapes with uniform particle size distribution. EE and DL of TP@PCL-PEG-FA micelles were (85.7 ± 5.8)% and (1.8 ± 0.5)%. TP@PCL-PEG-FA micelles showed obvious sustained release effect. Compared with common non-targeted PCL-PEG micelles, the cellular uptake efficiency of PCL-PEG-FA micelles in LPS-stimulated RAW 264.7 cells was significantly enhanced, and TP@PCL-PEG-FA has stronger in vitro anti-inflammatory effect. Conclusion TP@PCL-PEG-FA micelles targeting folate receptors are prepared, and have better targeted anti-inflammatory effect in vitro, which provides a new strategy and new idea for the nano-delivery system of triptolide.

R944

四川省中医药管理局中医药科研专项课题（2021MS206）；四川省骨科医院科研项目（2019ZD04）