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Influences of different sugar ligands on targeted delivery of liposomes.
Journal of Drug Targeting ( IF 4.3 ) Pub Date : 2020-04-13 , DOI: 10.1080/1061186x.2020.1744156
Changmei Zhang 1 , Zhong Chen 1 , Wenhua Li 1 , Xiaoying Liu 1 , Shukun Tang 1 , Lei Jiang 1 , Minghui Li 1 , Haisheng Peng 1 , Mingming Lian 1
Affiliation  

Ligands are an important part of targeted drug delivery systems. Optimised lignads not only improve the target efficiency, but also enhance therapeutical effect of drugs. In our research, five sugar molecules (Mannose, Galactose, Glucose, Malt disaccharide, and Maltotriose) conjugated PEG600-DSPE were synthesised, of which polysaccharides were first discovered by us as sugar ligands to modify liposomes, which interacts with over expressive GLUT on cancer cells. DiO was encapsulated as fluorescent probe to evaluate their cellular uptake abilities of targeting C6 glioma cells, and the distribution in different visceral organs of rats. The results demonstrated that Malt disaccharide and Glucose-PEG600-DSPE had the strong efficiency of cellular uptake by C6 glioma cells. The distribution and accumulation of liposomes showed that different sugars modified liposomes could target different visceral organs in rats. It has provided a novel idea for ligand selectivity and optimisation of nanocarriers for tumour targeted therapy.



中文翻译:

不同糖配体对脂质体靶向递送的影响。

配体是靶向给药系统的重要组成部分。优化的配体不仅可以提高靶向效率,还可以增强药物的治疗效果。在我们的研究中,我们合成了五种糖分子(甘露糖、半乳糖、葡萄糖、麦芽二糖和麦芽三糖)结合 PEG 600 -DSPE,其中多糖是我们首先发现的作为修饰脂质体的糖配体,与过度表达的 GLUT 相互作用。癌细胞。DiO 被封装为荧光探针,以评估其靶向 C6 胶质瘤细胞的细胞摄取能力,以及在大鼠不同内脏器官中的分布。结果表明麦芽二糖和葡萄糖-PEG 600-DSPE对C6神经胶质瘤细胞的细胞摄取具有很强的效率。脂质体的分布和积累表明不同糖类修饰的脂质体可以靶向大鼠不同的内脏器官。它为配体选择性和优化用于肿瘤靶向治疗的纳米载体提供了新思路。

更新日期:2020-04-13
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