丹酚酸B立方液晶纳米粒的制备及大鼠在体肠吸收

Study on preparation of cubic liquid crystalline nanoparticles of salvianolic acid B and intestinal absorption in situ in rats

[目的]以丹酚酸B(salB)为模型药物制备立方液晶纳米粒,并对其大鼠在体肠吸收进行考察。[方法]采用高压均质法制备丹酚酸B立方液晶纳米粒,以粒径、包封率为指标进行处方优化;透射电镜观察其形态;单向灌流法考察其大鼠在体肠吸收。[结果]纳米粒平均粒径为(172.2±5)nm,Zeta电位为(-14.8±2)mV,包封率为(38.6±3)%。肠吸收实验表明丹酚酸B溶液与纳米粒在全肠段均有吸收,且在十二指肠吸收最好,纳米粒的大鼠小肠吸收优于丹酚酸B溶液(P<0.05)。[结论]丹酚酸B立方液晶纳米粒能够促进其在大鼠小肠的吸收。

[Objective] To prepare salvianolic acid B-loaded cubic liquid crystalline nanoparticles （sal-B LCN ） and investigate the intestinal absorption character in situ in rats. [Methods] The nanoparticles were prepared using high-pressure homogenization. The prescription were optimized with drug size and entrapment efficiency were served as indexes. It＇s morphology was examined by transmission electron microscope and single pass perfusion method was used for its intestinal absorption character in situ in rat. [Results] The size of the nanoparticles was （172.2±5） nm, the zeta was （-14.8±2） mV and the entrapment efficiency was （38.6±3）%. The result suggested that sal-B solution and sal-B LCN could be absorbed at each intestinal segment and all the two preparations showed a maximum absorptions at the duodenum. The intestinal absorption of sal-B LCN was better than sal-B solution （P〈0.05）. [Conclusion] Sal-B LCN can improve the intestinal absorption of sal-B in rats.