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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