姜黄素装载的混合聚合物胶束物理表征、体外释放及药代动力学研究  

Physical Characterization in Vitro Release and Pharmacokinetic Studies of Curcumin-loaded Mixed Polymer Micelles

作　　者：王勇平 黄福满 汪新娌 黄小英 梁新丽 WANG Yongping;HUANG Fuman;WANG Xinli;HUANG Xiaoying;LIANG Xinli(Jiangxi Youmei Pharmaceutical Co.,LTD.,Wuyuan 333200,China;Key Laboratory of Modern TCM Preparations of Ministry of Education,Jiangxi University of Chinese Medicine,Nanchang 330004,China)

机构地区：[1]江西佑美制药有限公司,江西婺源333200 [2]江西中医药大学现代中药制剂教育部重点实验室,南昌330004

出　　处：《江西中医药大学学报》2025年第1期82-87,共6页Journal of Jiangxi University of Chinese Medicine

基　　金：现代中药制剂教育部重点实验室开放基金项目(Zdsys-202307)。

摘　　要：目的:制备姜黄素(Cur)载入氢化蓖麻油聚氧乙烯醚RH 40(Cremophor■RH 40,Cr RH 40)/普朗尼克F127混合纳米胶束(MMs),并对其物理性质及在大鼠体内的药代动力学进行评价。方法:采用薄膜分散法制备Cur-Cr RH 40/F127-MMs,并对其粒径、包封率、形态等进行表征;将12只SD大鼠随机分为姜黄素原料药0.5%CMC-Na混悬液(Cur-API)组和姜黄素纳米胶束(Cur-MMs)组,分别在给药后0.083、0.25、0.5、0.75、1、1.5、2、3、4、6、8、12 h于大鼠眼眶处静脉取血。采用LC-MS测定血药浓度,比较两组间药代动力学参数。结果:载姜黄素纳米胶束的载药量为(12.78±0.31)%,包封率为(89.43±3.07)%,平均粒径为(17.23±1.02)nm,PDI为0.153±0.007,Zeta电位为(-9.62±0.13)mV,具有球形微观结构;体外释放药物研究结果显示Cur-Cr RH 40/F127-MMs 96 h累积释放率显著高于Cur-API,具有良好的缓释性能;大鼠药代动力学研究结果显示,与Cur-API组比较,Cur-MMs组的C_(max)、AUC_(0-t)、AUC_(0-∞)明显增加,T_(max)显著延长,T_(1/2)缩短。结论:姜黄素胶束能显著增加姜黄素的生物利用度,延长达峰时间和缩短半衰期。Objective:Curcumin(Cur)was prepared and loaded into hydrogenated castor oil poly oxyethylene ether RH 40(Cremophor)■RH 40,Cr RH40)/Planck F127 mixed nano micelles(MMS),and their physical properties and pharmacokinetics in rats were evaluated.Methods:Cur-Cr RH 40/F127-MMs were prepared by thin film dispersion method,and their particle size,encapsulation efficiency and morphology were characterized.Twelve SD rats were randomly divided into curcumin API 0.5%CMC-Na suspension(Cur-API)group and curcumin nano micelles(Cur-MMs)group.Blood was taken from the orbital vein at 0.083,0.25,0.5,0.75,1,1.5,2,3,4,6,8 and 12 hours after administration.The plasma concentration was determined by LC-MS,and the pharmacokinetic parameters between the two groups were compared.Results:The drug loading capacity of curcumin-loaded nano micelles was(12.78±0.31)%,the encapsulation efficiency was(89.43±3.07)%,the average particle size was(17.23±1.02)nm,the PDI was 0.153±0.007,and the Zeta potential was(-9.62±0.13)mV,has a spherical microstructure.The results of 96h in vitro drug release showed that cur CR RH 40/f127 MMS had a significantly higher cumulative release rate than cur API,and had good sustained-release performance.The results of pharmacokinetics in rats showed that compared with Cur-API Group,the C_(max),AUC_(0-t) and AUC_(0-∞) of Cur-MMs group increased significantly,Tmax was significantly delayed,and T1/2 was shortened.Conclusion:Curcumin micelles can significantly increase the bioavailability of curcumin,prolong the peak time and shorten the half-life.

关 键 词：姜黄素 混合纳米胶束 物理表征 药代动力学 

分 类 号：R285[医药卫生—中药学]