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Desirable PEGylation for improving tumor selectivity of hyaluronic acid-based nanoparticles via low hepatic captured, long circulation times and CD44 receptor-mediated tumor targeting.
Nanomedicine: Nanotechnology, Biology and Medicine ( IF 4.2 ) Pub Date : 2019-11-15 , DOI: 10.1016/j.nano.2019.102105
Chao Teng 1 , Zhuodong Chai 1 , Zhongyue Yuan 2 , Lianjie Ren 3 , Chenshi Lin 1 , Zhen Yan 1 , Wei He 1 , Chao Qin 1 , Lei Yang 1 , Xiaopeng Han 1 , Lifang Yin 1
Affiliation  

PEG coating was regarded as one effective method to improve the tumor-targeting efficiency of hyaluronic acid-based nanoparticles (HBN). However, the research of interaction between PEG coating and different receptors such as stabilin-2 and CD44 was limited. Herein, we synthesized a series of PEGylated hyaluronic acid with Curcumin (PHCs) to evaluate the role of PEG coating density in the interaction between HA and its receptors, which influenced tissues targeting activity, pharmacokinetic profiles and therapeutic efficacy of HBN. Compared with other counterparts, PHC HBN with about 5% PEG coating density preferably accumulated in the tumor mass, rather than in the liver, and hold desirable anti-cancer effect. These results indicated that to obtain optimized anticancer effect of HBN, the cellular uptake efficiency between different types of the cells should be carefully balanced by different PEG densities.

中文翻译:

理想的PEG化可通过低肝捕获,长循环时间和CD44受体介导的肿瘤靶向改善透明质酸基纳米颗粒的肿瘤选择性。

PEG涂层被认为是提高透明质酸基纳米颗粒(HBN)的肿瘤靶向效率的一种有效方法。然而,PEG涂层与不同受体如stabilin-2和CD44之间相互作用的研究是有限的。在这里,我们合成了一系列的姜黄素(PHCs)聚乙二醇化的透明质酸,以评估PEG涂层密度在HA及其受体之间的相互作用中的作用,这影响了组织的靶向活性,药代动力学特征和HBN的治疗功效。与其他同类药物相比,具有约5%PEG涂层密度的PHC HBN优选在肿瘤块而不是肝脏中积累,并具有理想的抗癌作用。这些结果表明,要获得最佳的HBN抗癌作用,
更新日期:2019-11-15
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