An Ethylenediamine‐based Switch to Render the Polyzwitterion Cationic at Tumorous pH for Effective Tumor Accumulation of Coated Nanomaterials,Angewandte Chemie International Edition

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An Ethylenediamine‐based Switch to Render the Polyzwitterion Cationic at Tumorous pH for Effective Tumor Accumulation of Coated Nanomaterials
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2018-03-23 , DOI: 10.1002/anie.201801641
Abdul-Hackam Ranneh ₁ , Hiroyasu Takemoto ₁ , Shunya Sakuma ₁ , Aziz Awaad _{1,

2} , Takahiro Nomoto ₁ , Yuki Mochida ₃ , Makoto Matsui ₁ , Keishiro Tomoda ₁ , Mitsuru Naito ₄ , Nobuhiro Nishiyama _{1,

3}

Affiliation

Polyzwitterions are employed as coating polymers for biomaterials to induce an antifouling property on the surface. Fine‐tuning the betaine structure switches the antifouling property to be interactive with anionic tissue constituents in response to a tumorous pH gradient. The ethylenediamine moiety in the carboxybetaine enabled stepwise protonation and initiated the di‐protonation process around tumorous pH (6.5). The net charge of the developed polyzwitterion (PGlu(DET‐Car)) was thus neutral at pH 7.4 for antifouling, but was cationic at pH 6.5 for interaction with anionic constituents. Quantum dots coated with PGlu(DET‐Car) exhibited comparable stealth and enhanced tumor accumulation relative to the PEG system. The present study provides a novel design of smart switchable polyzwitterion based on a precise control of the net charge.

中文翻译：

一种基于乙二胺的开关，用于在pH值可变的情况下使聚两性离子阳离子呈现出来，从而有效地包覆了纳米材料，从而有效地积聚了肿瘤

聚两性离子被用作生物材料的涂层聚合物，以在表面上引发防污性能。甜菜碱结构的微调可切换防污性能，使其响应于肿瘤的pH梯度而与阴离子组织成分相互作用。羧基甜菜碱中的乙二胺部分能够逐步质子化，并在肿瘤pH值（6.5）附近启动了双质子化过程。因此，已开发的聚两性离子（PGlu（DET-Car））的净电荷在pH 7.4时呈中性以防污，但在pH 6.5时则与阳离子性组分相互作用时为阳离子。相对于PEG系统，涂有PGlu（DET-Car）的量子点具有可比的隐身性并增强了肿瘤积累。本研究提供了一种基于净电荷的精确控制的智能可切换多性两性离子的新颖设计。

更新日期：2018-03-23

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