目的 以姜黃多糖為穩(wěn)定劑制備口服姜黃素納米乳（curcumin nanoemulsion，Cur-NE），并對其進行表征及抗炎活性研究。方法 采用高壓均質法制備Cur-NE；以平均粒徑、多分散系數(shù)（polydispersity index，PDI）和ζ電位為考察指標，對比多種新型穩(wěn)定劑對Cur-NE的穩(wěn)定效果；并以油水體積比、乳化劑種類、油相種類、均質次數(shù)和均質壓力為考察因素，采用單因素實驗優(yōu)化處方工藝。利用激光衍射技術和透射電子顯微鏡對Cur-NE的粒徑、分布、穩(wěn)定性和形態(tài)進行表征。采用HPLC法檢測Cur-NE的載藥量、包封率以及體外釋放；并檢測Cur-NE的離心、酸堿、貯存穩(wěn)定性。構建細胞炎癥模型評價Cur-NE的抗炎活性。結果 5種穩(wěn)定劑中姜黃多糖的穩(wěn)定效果最佳。優(yōu)化后的處方工藝為姜黃多糖為穩(wěn)定劑，大豆油為油相、聚山梨酯80為乳化劑，油水體積比為1∶19，均質壓力為80.0 MPa（800 bar），均質次數(shù)為8次；制備的Cur-NE平均粒徑為（193.28±3.79）nm，PDI為0.112±0.013，ζ電位為（−27.77±1.31）mV，包封率為（87.08±0.79）%，載藥量為（0.111±0.007）mg/mL，且具有緩釋效應。Cur-NE呈均一的圓球形，離心穩(wěn)定性、酸堿穩(wěn)定性和貯存穩(wěn)定性均良好。Cur-NE可顯著抑制脂多糖誘導的RAW 264.7細胞釋放一氧化氮，且效果優(yōu)于姜黃多糖。結論 以姜黃多糖為穩(wěn)定劑制備的Cur-NE性質良好，且具有潛在的抗炎作用。

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

四川省科技計劃重點研發(fā)項目（2020YFN0152）