Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University, 1-1 Gakuen-cho, Naka-ku, Sakai, Osaka 599-8531, Japan.
Institute for Materials Chemistry and Engineering, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan.
Mater Sci Eng C Mater Biol Appl. 2021 Jul;126:112159. doi: 10.1016/j.msec.2021.112159. Epub 2021 May 1.
It has been reported that the amount of intermediate water, defined as water molecules loosely bound to a material, is a useful index of the material's bio-inert properties. Polyethylene glycol (PEG) is a well-known biocompatible polymer with a large amount of intermediate water. Many researchers have showed that PEGylated nanoparticles are passively accumulated in tumor tissues owing to their enhanced permeability and retention (EPR) effects. Dendrimers are regularly branched polymers with highly controllable size and structure, which can be exploited as potent drug carriers. In this study, we investigated the tripartite relationship among the PEG density, the hydration state, and the passive tumor targeting property, using PEGylated dendrimers. The fully PEGylated dendrimer, PEG64-den, showed similar hydration behavior to PEG and a passive tumor targeting property. In contrast, the hydration state of the partly PEGylated dendrimer, PEG5-den, was different from that of PEG64-den, and the passive tumor targeting property was not observed. This is the first report to show the hydration state of a drug carrier as well as discuss a relationship between the hydration state and biodistribution.
据报道，中间水的量（定义为与材料松散结合的水分子）是材料生物惰性特性的有用指标。聚乙二醇（PEG）是一种众所周知的生物相容性聚合物，具有大量的中间水。许多研究人员表明，由于具有增强的通透性和保留（EPR）效应，PEG 化纳米颗粒会被动地在肿瘤组织中积累。树枝状聚合物是具有高度可控尺寸和结构的规则支化聚合物，可用作有效的药物载体。在这项研究中，我们使用 PEG 化树枝状聚合物研究了 PEG 密度、水合状态和被动肿瘤靶向特性之间的三分关系。完全 PEG 化的树枝状聚合物 PEG64-den 表现出与 PEG 相似的水合行为和被动肿瘤靶向特性。相比之下，部分 PEG 化的树枝状聚合物 PEG5-den 的水合状态与 PEG64-den 不同，也没有观察到被动肿瘤靶向特性。这是第一个报告显示药物载体的水合状态并讨论水合状态与生物分布之间关系的研究。
