目的 以姜黄多糖为稳定剂制备口服姜黄素纳米乳（curcumin nanoemulsion，Cur-NE），并对其进行表征及抗炎活性研究。方法 采用高压均质法制备Cur-NE；以平均粒径、多分散系数（polydispersity index，PDI）和ζ电位为考察指标，对比多种新型稳定剂对Cur-NE的稳定效果；并以油水体积比、乳化剂种类、油相种类、均质次数和均质压力为考察因素，采用单因素实验优化处方工艺。利用激光衍射技术和透射电子显微镜对Cur-NE的粒径、分布、稳定性和形态进行表征。采用HPLC法检测Cur-NE的载药量、包封率以及体外释放；并检测Cur-NE的离心、酸碱、贮存稳定性。构建细胞炎症模型评价Cur-NE的抗炎活性。结果 5种稳定剂中姜黄多糖的稳定效果最佳。优化后的处方工艺为姜黄多糖为稳定剂，大豆油为油相、聚山梨酯80为乳化剂，油水体积比为1∶19，均质压力为80.0 MPa（800 bar），均质次数为8次；制备的Cur-NE平均粒径为（193.28±3.79）nm，PDI为0.112±0.013，ζ电位为（−27.77±1.31）mV，包封率为（87.08±0.79）%，载药量为（0.111±0.007）mg/mL，且具有缓释效应。Cur-NE呈均一的圆球形，离心稳定性、酸碱稳定性和贮存稳定性均良好。Cur-NE可显著抑制脂多糖诱导的RAW 264.7细胞释放一氧化氮，且效果优于姜黄多糖。结论 以姜黄多糖为稳定剂制备的Cur-NE性质良好，且具有潜在的抗炎作用。

Objective To prepare oral curcumin nanoemulsion (Cur-NE) with turmeric polysaccharide as stabilizer, and characterize it as well as study its anti-inflammatory activity. Methods Cur-NE was prepared by high-pressure homogenization method; the average particle size, polydispersity index (PDI) and ζ potential were used as indexes to compare the stabilizing effects of several novel stabilizers on Cur-NE; and the oil-water volume ratio, emulsifier type, oil phase type, homogenization number and homogenization pressure were also examined as factors to optimize the prescription process by single factor experiment. Particle size, distribution, stability and morphology of Cur-NE were characterized by laser diffraction and transmission electron microscopy. High performance liquid chromatography (HPLC) was used to measure the drug loading, encapsulation rate, and in vitro release of Cur-NE. The centrifugal stability, acid-base stability and storage stability of Cur-NE were determined. Meanwhile, a cellular inflammation model was constructed to evaluate the anti-inflammatory activity of Cur-NE. Results Among the five stabilizers, turmeric polysaccharide had the best stabilizing effect. The optimized process parameters were as follows: the stabilizer was turmeric polysaccharide, the oil phase was soybean oil, the emulsifier was Tween 80, the oil-water ratio was 1:19, the homogenization pressure was 80.0 MPa (800 bar), and the homogenization number was eight times. The average particle size of Cur-NE was (193.28 ± 3.79) nm, the PDI was 0.112 ± 0.013, the ζ potential was (−27.77 ± 1.31) mV, the encapsulation rate was (87.08 ± 0.79) %, the drug loading capacity was (0.111 ± 0.007) mg/mL, and it had a slow-release effect. Cur-NE presented a spherical shape with a uniform distribution, with the good centrifugal, acid-base and storage stability. Cur-NE significantly inhibited NO release from LPS-induced RAW 264.7 cells, and the effect was better than turmeric polysaccharide. Conclusion Cur-NE prepared with turmeric polysaccharide as stabilizer has good properties and potential anti-inflammatory effect.

R283.6

四川省科技计划重点研发项目（2020YFN0152）