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An Ethylenediamine‐based Switch to Render the Polyzwitterion Cationic at Tumorous pH for Effective Tumor Accumulation of Coated Nanomaterials |
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| Authors: | Abdul‐Hackam Ranneh Dr Hiroyasu Takemoto Shunya Sakuma Dr Aziz Awaad Dr Takahiro Nomoto Dr Yuki Mochida Dr Makoto Matsui Dr Keishiro Tomoda Dr Mitsuru Naito Prof Dr Nobuhiro Nishiyama |
| Institution: | 1. Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, Yokohama, Kanagawa, Japan;2. Department of Zoology, Faculty of Science, Sohag University, Naser City, Sohag, Egypt;3. Innovation Center of NanoMedicine (iCONM), Kawasaki Institute of Industrial Promotion, Kawasaki-ku, Kawasaki, Japan;4. Center for Disease Biology and Integrative Medicine, Graduate School of Medicine, The University of Tokyo, Bunkyo-ku, Tokyo, Japan |
| Abstract: | 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. |
| Keywords: | betaines net charge pH-responsiveness polymers targeted delivery |