タイトル |
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en
A pH-sensitive cationic lipid facilitates the delivery of liposomal siRNA and gene silencing activity in vitro and in vivo
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作成者 |
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アクセス権 |
open access |
主題 |
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Other
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Multifunctional envelope-type nano device (MEND)
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Other
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siRNA delivery
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Other
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pH-sensitive cationic lipid
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Other
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Intracellular trafficking
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Other
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Endosomal escape
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NDC
499
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内容注記 |
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Abstract
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Modification of liposomal siRNA carriers with polyethylene glycol, i.e., PEGylation, is a generally accepted strategy for achieving in vivo stability and delivery to tumor tissue. However, PEGylation significantly inhibits both cellular uptake and the endosomal escape process of the carriers. In a previous study, we reported on the development of a multifunctional envelope-type nano device (MEND) for siRNA delivery and peptide-based functional devices for overcoming the limitations and succeeded in the efficient delivery of siRNA to tumors. In this study, we synthesized a pH-sensitive cationic lipid, YSK05, to overcome the limitations. The YSK05-MEND had a higher ability for endosomal escape than other MENDs containing conventional cationic lipids. The PEGylated YSK05-MEND induced efficient gene silencing and overcame the limitations followed by optimization of the lipid composition. Furthermore, the intratumoral administration of the YSK05-MEND resulted in a more efficient gene silencing compared with MENDs containing conventional cationic lipids. Collectively, these data confirm that YSK05 facilitates the endosomal escape of the MEND and thereby enhances the efficacy of siRNA delivery into cytosol and gene silencing.
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出版者 |
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Elsevier B.V.
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日付 |
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言語 |
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資源タイプ |
journal article |
出版タイプ |
AM |
資源識別子 |
HDL
http://hdl.handle.net/2115/51165
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関連 |
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isVersionOf
DOI
https://doi.org/10.1016/j.jconrel.2012.09.009
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PMID
23000694
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収録誌情報 |
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Journal of Controlled Release
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巻163
号3
開始ページ267
終了ページ276
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ファイル |
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コンテンツ更新日時 |
2023-07-26 |