大黄酚白蛋白纳米粒的制备及其体内药动学研究  

Preparation and in vivo pharmacokinetics of chrysophanol albumin nanoparticles

作　　者：辛娟 易华 谈秀凤 丁玉[1] XIN Juan;YI Hua;TAN Xiu-feng;DING Yu(Huanghe Science and Technology College,Zhengzhou 450063,China;Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)

机构地区：[1]黄河科技学院,河南郑州450063 [2]上海中医药大学,上海201203

出　　处：《中成药》2021年第6期1399-1404,共6页Chinese Traditional Patent Medicine

摘　　要：目的制备大黄酚白蛋白纳米粒,并考察其体内药动学。方法采用牛血清白蛋白制备大黄酚白蛋白纳米粒,测定包封率、载药量、粒径、Zeta电位、溶解度、体外释药,透射电镜观察形态。大鼠随机分为2组,分别灌胃给予大黄酚及其白蛋白纳米粒0.5%CMC-Na混悬液(20 mg/kg),于0.5、1、1.5、2、3、4、5、6、8、10、12 h采血,HPLC法测定大黄酚血药浓度,计算主要药动学参数。结果所得白蛋白纳米粒呈球形,包封率为(93.61±1.02)%,载药量为(12.19±1.03)%,平均粒径为(156.5±6.7)nm, PDI为0.028±0.007,Zeta电位为(-35.1±3.8)mV,溶解度为(34.75±0.92)μg/mL,48 h内累积释放度为74.81%。与原料药比较,白蛋白纳米粒T_(max)缩短(P<0.05),C_(max)、AUC_(0~_t)、AUC_(0~∞)升高(P<0.01),生物利用度增加至4.02倍。结论白蛋白纳米粒可促进大黄酚体外溶出,提高其生物利用度。AIM To prepare chrysophanol albumin nanoparticles and to investigate their in vivo pharmacokinetics.METHODS Bovine serum albumin was employed to prepare chrysophanol albumin nanoparticles,after which the encapsulation efficiency,drug loading,particle size,Zeta potential,dissolution rate and in vitro drug release were determined,and the morphology was observed under transmission electron microscopy.Rats were randomly assigned into two groups and given intragastric administeration of the 0.5%CMC-Na suspensions of chrysophanol and its albumin nanoparticles(20 mg/kg),respectively,after which blood collection was performed at 0.5,1,1.5,2,3,4,5,6,8,10,12 h.HPLC was adopted in the plasma concentration determination of albumin,and the main pharmacokinetic parameters were calculated.RESULTS The spherical albumin nanoparticles demonstrated the encapsulation efficiency,drug loading,particle size,PDI,Zeta potential,dissolution rate and accumulative release rate within 48 h of(93.61±1.02)%,(12.19±1.03)%,(156.5±6.7)nm,0.028±0.007,(-35.1±3.8)mV,(34.75±0.92)μg/mL and 74.81%,respectively.Compared with the raw medicine,the albumin nanoparticles displayed shortened T_(max)(P<0.05)and increased C_(max),AUC_(0-t),AUC_(0-∞)(P<0.01),and the bioavailability was enhanced to 4.02 times.CONCLUSION Albumin nanoparticles can promote the in vitro dissolution of chrysophanol and enhance its bioavailability.

关 键 词：大黄酚 白蛋白纳米粒 制备 体内药动学 HPLC 

分 类 号：R944[医药卫生—药剂学]