黄芩苷固体脂质纳米粒的药代动力学和体外对肝癌细胞生长研究

摘要

Objective: To investigate the pharmacokinetics of baicalin solid lipid nanoparticals (BSLNs) in rats by HPLC method, and the inhibitory effect of BSLNs on the Hep G-2 cells.Method: By intravenous administration, the concentration of baicalin in blood plasma at different time points were determined.Human Hep G-2 cells were treated with BSLNs, and the effects on cells inhibition were investigated by CCK-8 cell viability assay.Result: The study of pharmacokinetics of BSLNs and baicalins-sol in rats showed that the two preparations were fitted with two-compartment model;and pharmacokinetic results showed that the mean AUC0-t of BSLNs group was 350.751μg/mL, t1/2 is 5.983h, while the AUC=231.178μg/mL, t1/2 beta=4.434h.(Weighting factor is1/C2).The absolute bioavailability was 163.394%.Conclusion: BSLNs group shows a significant sustained-release in vivo.Then BSLNs shows a greater effect on inhibiting the growth of Hep G-2 cells compared with baicalins-sol group.%目的:采用高效液相色谱法研究黄芩苷固体脂质纳米粒在大鼠体内的药物动力学特征,观察黄芩苷固体脂质纳米粒在体外对肝癌细胞生长影响. 方法:采用大鼠尾静脉注射给药,测定不同时间点大鼠体内的血药浓度.采用CCK-8法测定黄芩苷固体脂质纳米粒溶液体外抑制Hep G-2细胞的生长情况.结果:黄芩苷固体脂质纳米粒溶液和黄芩苷溶液组在大鼠体内均符合药动学二室模型(权重系数为1/C2),且黄芩苷固体脂质纳米粒溶液组平均AUC0-t=350.751μg/mL,t1/2=5.983h,baicalin溶液组AUC=231.178μg/mL,t1/2 beta=4.434h,黄芩苷固体脂质纳米粒溶液在体内的绝对生物利用度为163.394%.结论:黄芩苷固体脂质纳米粒溶液在大鼠体内具有缓释作用,且黄芩苷固体脂质纳米粒溶液体外对Hep G-2细胞的生长有抑制作用,并且抑制作用强于黄芩苷溶液组.