白杨素纳米结构脂质载体制备及大鼠体内药动学

Preparation and Pharmacokinetic of Nanostructured Lipid Carrier of Chrysin in Rat

目的制备白杨素纳米结构脂质载体,并比较其与白杨素经SD大鼠灌胃给药后体内药动学及生物利用度的差异。方法采用微射流均质法制备,正交实验优化白杨素纳米结构脂质载体的处方,对粒径、Zeta电位和体外释放情况进行考察。将12只SD大鼠随机分为白杨素原料药组和白杨素纳米结构脂质载体组,给药剂量为50 mg·kg-1。高效液相色谱(HPLC)法测定血药浓度,计算主要药动学参数。结果白杨素纳米结构脂质载体最佳处方包封率为(84.92±1.38)%,载药量为(7.22±0.31)%,平均粒径为(217.42±11.06)nm,Zeta电位为(-30.4±3.6)mV。体外释放研究结果显示白杨素纳米结构脂质载体在体外具有明显的缓释特征。口服药动学研究结果显示,白杨素纳米结构脂质载体相对生物利用度提高至3.10倍。结论白杨素纳米结构脂质载体可显著促进白杨素体内吸收,提高生物利用度。

Objective To prepare chrysin nanostructured lipid carrier,and to compare its oral bioavailability and pharmacokinetics with chrysin suspension after intragastric administration in SD rats.Methods The microjet homogeneity method was employed to optimize the preparation of chrysin nanostructured lipid carrier using orthogonal test.The particle size,Zeta potential,and in vitro drug release profile were also investigated.Twelve SD rats were randomly divided into chrysin suspension group and chrysin nanostructured lipid carrier group,and the dosage of intragastric administration was 50 mg·kg-1.HPLC was used to determine the plasma concentration of chrysin and the main pharmacokinetic parameters were also been calculated.Results The encapsulation efficiency,drug loading,particle size,and Zeta potential of the optimized chrysin nanostructured lipid carrier were(84.92±1.38)%,(7.22±0.31)%,(217.42±11.06)nm,and(-30.4±3.6)mV,respectively.Chrysin nanostructured lipid carrier had obvious sustained release characteristics compared to chrysin suspension.The results of oral pharmacokinetics showed that the relative bioavailability of chrysin nanostructured lipid carrier was increased 3.10 times.Conclusion Chrysin nanostructured lipid carries could promote the absorption and improve the bioavailability of chrysin significantly.