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Synthesis of high functionality and quality mannose-grafted lipids to produce macrophage-targeted liposomes


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タイトル: Synthesis of high functionality and quality mannose-grafted lipids to produce macrophage-targeted liposomes
著者: Hagimori, Masayori / Chinda, Yorinao / Suga, Tadaharu / Yamanami, Kazuto / Kato, Naoya / Inamine, Tatsuo / Fuchigami, Yuki / Kawakami, Shigeru
発行日: 2018年10月15日
出版者: Elsevier B.V.
引用: European Journal of Pharmaceutical Sciences, 123, pp.153-161; 2018
抄録: The mannose receptor, which is responsible for tumor invasion, proliferation, and metastasis in the tumor microenvironment, is overexpressed in tumor-associated macrophages. Mannose is commonly applied to PEGylated liposomes in macrophage-targeted cancer therapy. To develop a high functionality and quality (HFQ) lipid for macrophage-targeted liposomes, we designed a novel mannosylated lipid with improved mannose receptor binding affinity using serine–glycine repeats (SG)n. We synthesized Man(S)-(SG)5-SSK-K(Pal)2 using only a fluorenylmethyloxycarbonyl (Fmoc) protecting group solid-phase peptide synthesis method, which produced a high-quality lipid at a moderately good yield. We then prepared Man-(SG)5/PEGylated liposomes using a post-insertion technique to insert Man(S)-(SG)5-SSK-K(Pal)2 into the PEGylated liposomes. In vitro cell investigations revealed that the Man-(SG)5/PEGylated liposomes effectively associated with mouse peritoneal macrophages by interacting with the mannose receptors. The results suggest that we produced a novel high-quality, highly functional mannosylated lipid that is suitable for clinical drug delivery applications.
キーワード: Lipid / Liposome / Macrophage / Mannose / Serine–glycine repeat spacer
URI: http://hdl.handle.net/10069/38547
ISSN: 09280987
DOI: 10.1016/j.ejps.2018.07.036
権利: © 2018 Elsevier B.V. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
資料タイプ: Journal Article
原稿種類: author
出現コレクション:110 学術雑誌論文

引用URI : http://hdl.handle.net/10069/38547

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