姜酮纳米混合胶束的制备及其对高脂血症的调节作用  

Preparation of zingerone nano-mixed micelles and its regulating effect on hyperlipidemia

作　　者：葛竹妹 余江南[1] 徐希明[1] GE Zhumei;YU Jiangnan;XU Ximing(College of Pharmacy,Jiangsu University,Zhenjiang Jiangsu 212013,China)

机构地区：[1]江苏大学药学院,江苏镇江212013

出　　处：《江苏大学学报（医学版）》2022年第1期72-79,共8页Journal of Jiangsu University：Medicine Edition

基　　金：国家自然科学基金资助项目(81773695)。

摘　　要：目的:研究纳米混合胶束包载姜酮后对高脂血症的影响。方法:采用薄膜分散法制备姜酮纳米混合胶束(zingerone nano-mixed micelles,ZNMs),通过单因素和正交试验对处方进行优化筛选,测定其表观形态、粒径、载药量和包封率。用油酸诱导人肝癌细胞脂质蓄积以及高脂饲料喂养小鼠建立高脂模型,分析ZNMs对高血脂的调节作用。结果:ZNMs的最优处方是投药量为40 mg,m_(磷脂)∶m_(胆酸钠)=2∶3,聚乙烯吡咯烷酮K3(PVP K30)用量为30 mg,维生素E聚乙二醇琥珀酸酯(TPGS)用量为22 mg。制得的ZNMs粒径为(50.62±0.25)nm,包封率(94.71±2.02)%。体外释放实验表明,ZNMs累计释放率明显高于原料药。ZNMs能降低高脂饲料引起的高脂血症小鼠血脂代谢,也能影响油酸诱导的细胞脂质蓄积,与姜酮组相比,ZNMs组血脂水平明显改善(P<0.05)。结论:纳米混合胶束对姜酮起到良好的增溶作用,提高抗高血脂效能,且能在生物体内发挥作用。Objective:To evaluate the effect of zingerone-loaded nano-mixed micelles on hyperlipidemia.Methods:The thin film dispersion method was used to prepare zingerone nano-mixed micelles(ZNMs).The prescription was optimized and screened through single factor and orthogonal experiments,and the apparent morphology,particle size,drug loading and encapsulation efficiency were determined.Oleic acid was used to induce lipids in human liver cancer cells and high-fat diets were used to establish a high-fat model to analyze the effect of ZNMs on the regulation of hyperlipemia.Results:The optimal prescription for ZNMs is 40 mg,phospholipid∶sodium cholate 2∶3(m/m),polyvinylpyrrolidone K3(PVP K30)30 mg,and vitamin E polyethylene glycol succinate(TPGS)22 mg.The particle size of the prepared ZNMs is(50.62±0.25)nm,and the encapsulation efficiency is(94.71±2.02)%.In vitro release experiments showed that the cumulative release rate of ZNMs is significantly higher than that of the bulk drug.ZNMs could reduce blood lipid metabolism in hyperlipidemia mice caused by high-fat diet,and could also decrease cell lipid accumulation induced by oleic acid.Compared with the zingerone group,the blood lipid level of ZNMs group was significantly improved(P<0.05).Conclusion:Nano-mixed micelles enhance solubilization of zingerone,improve the anti-hyperlipidemia efficacy,and effectively come into effect in the whole organism.

关 键 词：姜酮 纳米混合胶束 脂质蓄积 高脂血症 

分 类 号：R589.2[医药卫生—内分泌] R965[医药卫生—内科学]