[关键词]
[摘要]
目的 采用人肝癌SMMC-7721细胞移植裸鼠,研究包载人参3种成分(齐墩果酸、熊果酸、人参皂苷Rg3,OUR)的透明质酸(hyaluronic acid,HA)修饰的纳米脂质载体(HA-OUR-NLC)在荷瘤小鼠体内的分布情况。方法 以FITC和DiR为荧光探针,采用荧光内窥式共聚焦成像和小动物活体成像技术动态监测HA-OUR-NLC靶向到各组织器官的行为过程。结果 HA-OUR-NLC可明显提高齐墩果酸、熊果酸、人参皂苷Rg3在肿瘤中的相对摄取率(RUE),分别达到2.51±1.23、2.27±1.43和2.77±0.25,表明经过HA修饰的纳米粒可增强药物在肿瘤中的摄取。DiR-HA-OUR-NLC组荷瘤裸鼠肿瘤区域可以明显观察到较强的荧光信号,显著高于DiR-OUR-NLC组。结论 HA-OUR-NLC能够在肝肿瘤部位富集,可明显提高给药系统的肿瘤靶向性。
[Key word]
[Abstract]
Objective Human hepatoma SMMC-7721 cells were transplanted into nude mice to study the tissue distribution of nanostructured lipid carrier modified by hyaluronic acid (HA-OUR-NLC) loaded with three components in Panax ginseng (oleanolic acid, ursolic acid, and ginsenosider Rg3, OUR). Methods FITC and DiR were used as fluorescent probes to dynamically monitor the HA-OUR-NLC targeted behavior of various tissues and organs through fluorescence endoscopic confocal imaging and in vivo imaging studies. Results RUE values of oleanolic acid, ursolic acid, and ginsenosider Rg3 in tumors were significantly increased in HA-OUR-NLC group, reaching 2.51 ±1.23, 2.27 ±1.43, and 2.77 ±0.25, respectively, which indicated that nanoparticles modified by hyaluronic acid could enhance drug uptake in tumors. The DiR accumulation in tumors of DiR-HA-OUR-NLC was higher than that of DiR-OUR-NLC by the visualized fluorescence of in vivo imaging. Conclusion It indicated that nanoparticles modified by hyaluronic acid loaded with three components in P. ginseng can be enriched in the tumor site of liver cancer, which is in line with the expectation and can significantly improve the tumor targeting of the drug delivery system.
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[基金项目]
国家自然科学基金青年基金项目(81803985);黑龙江省自然科学基金资助项目(H2016060)