オオサワ シゲヒト   Oosawa Shigehito
  大澤 重仁
   所属   医学研究科 医学研究科 (医学部医学科をご参照ください)
   職種   非常勤講師
論文種別 原著
言語種別 英語
査読の有無 査読あり
表題 Installation of a thermoswitchable hydrophobic domain into a unimer polyion complex for enhanced cellular uptake of siRNA
掲載誌名 正式名:Bioconjugate chemistry
略  称:Bioconjug Chem
ISSNコード:10431802/15204812
掲載区分国外
巻・号・頁 31(5),pp.1320-1326
総ページ数 7
著者・共著者 Beob Soo Kim, Shigehito Osawa, Jongmin Yum, Mitsuru Naito, Kanjiro Miyata
担当区分 2nd著者
発行年月 2020/04/30
概要 Whereas small siRNA nanocarriers with a size of 10–20 nm exert high tissue-permeability, they encounter the challenge of inefficient adsorption on the cell surface, resulting in poor cellular uptake of siRNA. To solve this dilemma, this study aims to control the hydrophobicity of a small siRNA nanocarrier, unimer polyion complex (uPIC), with a size of ∼10 nm. The uPICs are fabricated to consist of a single pair between siRNA and a smart triblock copolymer comprising hydrophilic poly(2-ethyl-2-oxazoline) (PEtOx), thermoswitchable poly(2-n-propyl-2-oxazoline) (PnPrOx), and cationic poly(l-lysine) (PLL). The PnPrOx segment is dehydrated at 37 °C (>lower critical solution temperature) to enhance the hydrophobicity of uPICs. The uPICs with a hydrophobic domain facilitates cellular uptake of the siRNA payload through stronger binding to the cell surface, compared with control uPICs without a PnPrOx segment, leading to a significantly enhanced gene silencing effect in cultured cancer cells.
DOI 10.1021/acs.bioconjchem.0c00238