毛菊苣总倍半萜磁性纳米脂质体在小鼠体内组织分布和靶向效果

目的研究毛菊苣总倍半萜有效部位、脂质体和磁性纳米脂质体在小鼠体内的组织分布和靶向效果。方法采用高效液相色谱法,以山莴苣素的含量为评价指标,研究毛菊苣总倍半萜有效部位溶液组、脂质体溶液组和磁性纳米脂质体溶液组(加磁场)在小鼠体内不同组织器官的药物浓度;并以AUC0-12 h、平均滞留时间(MRT)和靶向效率(TE)、相对靶向效率(RTE)、靶向指数(TI)为指标评价不同剂型的靶向作用。结果尾静脉注射给药10 min后,磁性纳米脂质体组在心、肝、脾、肺、肾脏组织中山莴苣素浓度较有效部位组、脂质体组显著提高;在动物的肝部体外施加磁场,磁性纳米脂质体组肝部位的AUC0-12 h明显高于其他部位,MRT明显的延长,差异具有显著性(P0.01);TE仅在肝部有增加,且TI大于10。结论在外加磁场的作用下,毛菊苣总倍半萜磁性纳米脂质体可改变药物在动物体内的分布,延长药物的作用时间,提高药物在肝部位的特异性和靶向性。

Tissue distribution and targeting of Magnetic Nano-liposomes of Sesquiterpene- Rich Fraction from Cichorium glandulosum in mice

Objective To study the tissue distribution and targeting of Sesquiterpene-Rich Fraction (SRF), Liposomes of Sesquiterpene-Rich Fraction (SRF-LP) and Magnetic Nano-liposomes of Sesquiterpene-Rich Fraction (SRF- MLN) in the mice. Methods HPLC method was used to determine the concentration of lactucin in tissue samples of mice. Taking the content of lactucin as the evaluation index, the concentration of SRF group, SRF-LP group, and SRF-MLN group (plus magnetic field) in different tissues and organs of mice was studied, and the targeting effects of different dosage forms were evaluated by AUC_{0-12 h}, MRT, TE, RTE, and TI. Results The concentration of SRF-MLN in heart, liver, spleen, lung and kidney tissues was significantly higher than that in the SRF and SRF-LP groups 10 min after tail vein injection. The magnetic field was applied to the liver of animals in vitro, and the AUC_{0-12 h} of SRF-MLN group was significantly higher than that of other parts, and the MRT was significantly prolonged (P<0.01). The TE was only increased in the liver, and TI was above 10. Conclusion Under the action of external magnetic field, SRF-MLN can change the distribution of drugs in animals, prolong action time of drugs, and improve specificity and targeting of drugs in liver.