目的 制備雷公藤甲素葉酸靶向納米膠束（TP@PCL-PEG-FA），并研究其體外抗炎效果。方法 采用薄膜水化法制備TP@PCL-PEG-FA膠束，對粒徑和電位進(jìn)行表征，觀察其形態(tài)特征，采用超濾法測定包封率和載藥量，同時考察藥物的體外釋放。觀察膠束的攝取效率，考察體外抗炎作用。結(jié)果 TP@PCL-PEG-FA膠束的平均粒徑為（34.1±5.1） nm，Zeta電位為（-10.1±2.2） mV，呈類球形，粒徑分布均一。包封率為（85.7±5.8）%，載藥量為（1.8±0.5）%。TP@PCL-PEG-FA膠束均能夠相對緩慢釋放藥物，具有緩釋效果。與普通非靶向PCL-PEG膠束相比，PCL-PEG-FA膠束在脂多糖刺激的RAW 264.7細(xì)胞中的攝取效率明顯提高，TP@PCL-PEG-FA膠束有更強(qiáng)的體外抗炎效率。結(jié)論 制備了雷公藤甲素的葉酸靶向的TP@PCL-PEG-FA膠束，具有更好的體外靶向抗炎作用，為雷公藤甲素的納米遞藥系統(tǒng)提供了一種新策略和新思路。

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

四川省中醫(yī)藥管理局中醫(yī)藥科研專項課題（2021MS206）；四川省骨科醫(yī)院科研項目（2019ZD04）