雷公藤甲素叶酸靶向纳米胶束的制备及其体外抗炎作用研究  

Preparation and in vitro anti-inflammatory effect of triptolide-loaded folic acidmodified micelles

作　　者：王润孔 肖焜壁 陈柯霏 WANG Run-kong;XIAO Kun-bi;CHEN Ke-fei(Preparation Center,Sichuan Provincial Orthopedic Hospital,Chengdu 610041,China)

机构地区：[1]四川省骨科医院制剂中心,四川成都610041

出　　处：《现代药物与临床》2023年第2期317-322,共6页Drugs & Clinic

基　　金：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)。

摘　　要：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-PEGFA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 antiinflammatory 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-PEGFA micelles in LPS-stimulated RAW 264.7 cells was significantly enhanced,and TP@PCL-PEG-FA has stronger in vitro antiinflammatory effect.Conclusion TP@PCL-PEG-FA micelles targeting folate receptors are prepared,and have better targeted antiinflammatory effect in vitro,which provides a new strategy and new idea for the nano-delivery system of triptolide.

关 键 词：雷公藤甲素叶酸靶向纳米胶束 粒径 雷公藤甲素 包封率 载药量 体外释放 摄取效率 抗炎作用 

分 类 号：R944[医药卫生—药剂学]