姜黄多糖为稳定剂制备口服姜黄素纳米乳及其抗炎活性研究  

Preparation of oral curcumin nanoemulsion with polysaccharides from Curcuma longa as stabilizer and its anti-inflammatory activity

作　　者：罗益蓉 王隽 朱宗萍 林丽婷 卿莹 陈元惠 李锐[1] 施婷 马云桐[1] 廖婉[1] LUO Yirong;WANG Jun;ZHU Zongping;LIN Liting;QING Ying;CHEN Yuanhui;LI Rui;SHI Ting;MA Yuntong;LIAO Wan(State Key Laboratory of SouthwesternChinese Medicine Resources,School of Pharmacy/School of Modern Chinese Medicine Industry,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Department of TCM Pharmacy,Chengdu Integrated TCM&Western Medicine Hospital,Chengdu 610041,China)

机构地区：[1]成都中医药大学西南特色中药资源国家重点实验室,药学院/现代中药产业学院,四川成都611137 [2]成都市中西医结合医院中药剂科,四川成都610041

出　　处：《中草药》2025年第6期1935-1944,共10页Chinese Traditional and Herbal Drugs

基　　金：四川省科技计划重点研发项目(2020YFN0152)。

摘　　要：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)andζpotential 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,theζpotential 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 antiinflamma

关 键 词：姜黄素 纳米乳 姜黄多糖 高压均质法 抗炎 缓释效应 

分 类 号：R283.6[医药卫生—中药学]