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目的评价水飞蓟素肠溶PLGA纳米粒口服给药后在大鼠体内的分布及肝靶向效率。方法以水飞蓟素分散片为对照,大鼠灌胃给药给予水飞蓟素肠溶PLGA纳米粒和水飞蓟素PLGA纳米粒后,采用高效液相色谱法测定血浆及各组织匀浆液中的药物浓度,采用DAS 3.0计算AUC值,以相对靶向效率(RTE)和肝靶向效率(TE)评价各制剂对肝脏的靶向性。结果以水飞蓟素分散片为对照,水飞蓟素肠溶PLGA纳米粒和水飞蓟素PLGA纳米粒给药后,血浆及各组织的RTE值均大于1,肝脏RTE值均大于10;两种纳米粒制剂给药后,肝脏相对于血浆及各组织TE值均大于1.5。结论水飞蓟素肠溶PLGA纳米粒大鼠给药后能有效提高其体内吸收和组织分布,具有良好的肝靶向作用。
Objective To evaluate the distribution and liver targeting efficiency of silymarin-loaded PLGA nanoparticles in rats after oral administration. Methods Silymarin dispersible tablets were used as control. After intragastric administration of silymarin-loaded PLGA nanoparticles and silymarin PLGA nanoparticles, the concentration of drug in plasma and tissue homogenates was determined by DAS 3.0 AUC values, the targeting of each formulation to the liver was evaluated in terms of relative targeting efficiency (RTE) and liver targeting efficiency (TE). Results Silymarin dispersible tablets as control, silymarin enteric PLGA nanoparticles and silymarin PLGA nanoparticles administered plasma and tissue RTE values were greater than 1, the liver RTE values were greater than 10; two kinds of nanoparticles after administration, Liver relative to plasma and each tissue TE values were greater than 1.5. Conclusion Silymarin enteric PLGA nanoparticles can improve the absorption and tissue distribution of PLGA nanoparticles in vivo and have good liver targeting effect.