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大澤 重仁
Department Research Institutes and Facilities, Research Institutes and Facilities Position |
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| Article types | Original article |
| Language | English |
| Peer review | Peer reviewed |
| Title | Installation of a thermoswitchable hydrophobic domain into a unimer polyion complex for enhanced cellular uptake of siRNA |
| Journal | Formal name：Bioconjugate chemistry Abbreviation：Bioconjug Chem ISSN code：10431802/15204812 |
| Domestic / Foregin | Foregin |
| Volume, Issue, Page | 31(5),pp.1320-1326 |
| Total page number | 7 |
| Author and coauthor | Beob Soo Kim, Shigehito Osawa, Jongmin Yum, Mitsuru Naito, Kanjiro Miyata |
| Authorship | 2nd author |
| Publication date | 2020/04/30 |
| Summary | 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 |