Preparation of novel butyryl galactose ester-modified coix component microemulsions and evaluation on hepatoma-targeting in vitro and in vivo
Preparation of novel butyryl galactose ester-modified coix component microemulsions and evaluation on hepatoma-targeting in vitro and in vivo
复制标题
新型丁酰半乳糖酯修饰薏苡仁组分微乳的制备及体内外肝癌靶向评价
DOI：
10.1080/10717544.2016.1189984
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发表时间：
2016-11-01
期刊：
影响因子：
6
通讯作者：
Ding, Xue Fang
中科院分区：
文献类型：
--
作者：
Liu, Ming Jian;Qu, Ding;Ding, Xue Fang
摘要：开发了丁基半乳糖酯修饰薏薏成分微乳（But-Gal-CMEs），以增强肝脏肿瘤特异性靶向性。该研究旨在评估体外和体内But-Gal-CMEs靶向肝癌的潜力。而均匀球形的- gal - cme粒径较小（56.68±0.07 nm），多分散性较窄（PDI为0.144±0.005），表面电荷略负（- 0.102±0.008 mV）。在细胞摄取研究中，But-Gal-CMEs对HepG2细胞模型的细胞内荧光强度有显著增强，相对于coix组分微乳（CMEs）提高了1.93倍。但- gal -CMEs对HepG2细胞的IC50为64.250 μg/mL，明显强于CMEs。在细胞凋亡研究中，与CMEs相比，50 μg/mL的But-Gal-CMEs使HepG2的凋亡细胞总数增加1.34倍。在体内生物分布研究中，负载cy5的But-Gal-CMEs的肿瘤内荧光比负载cy5的CMEs高1.43倍，表明其在肿瘤部位的积累明显增强。综上所述，But-Gal可以作为一种新型配体掺入尾骨成分微乳中，实现肝癌靶向药物的递送。
Abstract The butyryl galactose ester-modified coix component microemulsions (But-Gal-CMEs) was developed for enhanced liver tumor-specific targeting. The study was aimed to evaluate the hepatoma-targeting potential of But-Gal-CMEs in vitro and in vivo. But-Gal-CMEs with a uniform spherical shape exhibited a small particle size (56.68 ± 0.07 nm), a narrow polydispersity (PDI, 0.144 ± 0.005) and slightly negative surface charge (−0.102 ± 0.008 mV). In the cell uptake studies, But-Gal-CMEs showed a significant enhancement on the intracellular fluorescent intensity on HepG2 cells model, which was 1.93-fold higher relative to coix component microemulsions (CMEs). The IC50 of But-Gal-CMEs against HepG2 cells was 64.250 μg/mL, which was notably stronger than that of CMEs. In the cell apoptosis studies, compared with CMEs, But-Gal-CMEs (50 μg/mL) treatment resulted in a 1.34-fold rise in total apoptosis cells of HepG2. In the biodistribution studies in vivo, the intratumorous fluorescence of Cy5-loaded But-Gal-CMEs was 1.43-fold higher relative to that of Cy5-loaded CMEs, suggesting an obviously enhanced accumulation in the tumor sites. Taken as together, But-Gal could be incorporated into the coix component microemulsions as a novel ligand for realizing hepatoma-targeting drugs delivery.