芒果苷固体脂质纳米粒的制备及其体内药动学研究  

Preparation and in vivo pharmacokinetics of mangiferin solid lipid nanoparticles

作　　者：吕东霞 禹瑞 屈战果 范明松 LÜ Dong-xia;YU Rui;QU Zhan-guo;FAN Ming-song(Zhengzhou Shuqing Medical College,Zhengzhou 450064,China;Shanghai Leiyunshang Pharmaceutical Co.,Ltd.,Shanghai 201401,China)

机构地区：[1]郑州澍青医学高等专科学校,河南郑州450064 [2]上海雷允上药业有限公司,上海201401

出　　处：《中成药》2020年第11期2835-2839,共5页Chinese Traditional Patent Medicine

摘　　要：目的制备芒果苷固体脂质纳米粒,并考察其体内药动学。方法乳化-超声法制备固体脂质纳米粒,检测其形态、包封率、载药量、粒径、Zeta电位、体外释药。大鼠随机分为2组,分别灌胃给予芒果苷及其固体脂质纳米粒混悬液(20 mg/kg),于0.167、0.33、0.5、1、2、3、4、6、8、10、12 h采血,HPLC法测定芒果苷血药浓度,计算主要药动学参数。结果所得固体脂质纳米粒呈类球形或椭圆形,无粘连,平均包封率为80.61%,载药量为3.16%,粒径为178.63 nm,Zeta电位为-18.2 mV,4 h内累积释放度在90%以上,体外释药符合Weibull模型(R2=0.9725)。纳米粒tmax、Cmax、AUC0~t、AUC0~∞高于原料药(P<0.01),相对生物利用度提高至216.69%。结论固体脂质纳米粒可促进芒果苷体内吸收,提高其口服生物利用度,能作为该成分的药物递送系统。AIM To prepare mangiferin solid lipid nanoparticles and to investigate their in vivo pharmacokinetics.METHODS For the solid lipid nanoparticles prepared by emulsification-ultrasonic method,their morphology,encapsulation efficiency,drug loading,particle size,Zeta potential and in vitro drug release were detected.Rats were randomly assigned into two groups and given intragastric administration of the suspensions of mangiferin and its solid lipid nanoparticles(20 mg/kg),respectively,after which blood collection was performed at 0.167,0.33,0.5,1,2,3,4,6,8,10,12 h.HPLC was adopted in the plasma concentration determination of mangiferin,and the main pharmacokinetic parameters were calculated.RESULTS The obtained solid lipid nanoparticles were spherical-like or elliptical without adhesion,demonstrating the average encapsulation efficiency of 80.61%,drug loading of 3.16%,particle size of 178.63 nm,Zeta potential of-18.2 mV,and more than 90%of accumulative release rate within 4 h.The in vitro drug release accorded with Weibull model(R2=0.9725).The nanoparticles displayed higher tmax,Cmax,AUC0-t and AUC0-∞than the raw medicine(P<0.01),and the relative bioavailability was increased to 216.69%.CONCLUSION Solid lipid nanoparticles can promote the in vivo absorption of mangiferin and enhance its oral bioavailability,thus can be taken as the drug delivery system of this constituent.

关 键 词：芒果苷 固体脂质纳米粒 制备 体内药动学 乳化-超声法 HPLC 

分 类 号：R944[医药卫生—药剂学]