In the present study, the silibinin (SLB) was loaded into porous starch (PS) in the form of nanoparticles (SNPS) by the liquid antisolvent precipitation (LAP) method, so as to improve its solubility and bioavailability. Firstly, the different experimental parameters on drug loading (DL) of the SLB in the LAP process were optimized through the single-factor experiments. Under the optimum conditions, the DL and the encapsulation efficiency (EE) of the SNPS were 9.49 ± 0.37% and 89.93 ± 0.64%, respectively. Compared with free SLB and SLB nanoparticles (SN), the SNPS had a higher solubility, and was about 180.81 ± 5.32 μg/mL in artificial gastric juice (AGJ) and was about 88.91 ± 4.14 μg/mL in artificial intestinal juice (AIJ), respectively. The in vitro release study demonstrated a slow and sustained ± release of SLB from the SNPS with the SN and free SLB as controls. The pharmacokinetic results showed that the Cmax and AUC(0–t) of the SNPS (87.71 ± 7.24 μg/L, 439.55 ± 8.76 μg/L*h) increased when compared with the SN (60.31 ± 8.98 μg/L, 206.51 ± 12.24 μg/L*h) and free SLB (26.08 ± 1.43 μg/L, 102.63 ± 7.15 μg/L*h), showing its ability to improve SLB’s pharmacokinetic properties.

本研究通过液体抗溶剂沉淀（LAP）法将水飞蓟宾（SLB）以纳米颗粒（SNPS）的形式负载在多孔淀粉（PS）中，以提高其溶解度和生物利用度。首先，通过单因素实验优化了LAP过程中SLB载药量（DL）的不同实验参数。在最佳条件下，SNPS的DL和包封效率（EE）分别为9.49±0.37％和89.93±0.64％。与游离SLB和SLB纳米颗粒（SN）相比，SNPS的溶解度更高，在人造胃液（AGJ）中约为180.81±5.32μg/ mL，在人造肠液（AIJ）中约为88.91±4.14μg/ mL ， 分别。体外释放研究表明，以SN和游离SLB为对照，从SNPS缓慢且持续地释放SLB。药代动力学结果表明与SN（60.31±8.98μg/ L，206.51±12.24μg/ L * h）相比，SNPS的最大值和AUC （0-t）增加（87.71±7.24μg/ L，439.55±8.76μg/ L * h） ）和游离SLB（26.08±1.43μg/ L，102.63±7.15μg/ L * h），表明其具有改善SLB药代动力学特性的能力。