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Synthesis of a high functionality and quality lipid with gp130 binding hydrophobic peptide for the preparation of human glioma cell-targeted PEGylated liposomes


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タイトル: Synthesis of a high functionality and quality lipid with gp130 binding hydrophobic peptide for the preparation of human glioma cell-targeted PEGylated liposomes
著者: Suga, Tadaharu / Watanabe, Masanori / Sugimoto, Yuri / Masuda, Tomonari / Kuroda, Naotaka / Hagimori, Masayori / Kawakami, Shigeru
発行日: 2019年 2月
出版者: Elsevier B.V.
引用: Journal of Drug Delivery Science and Technology, 49, pp.668-673; 2019
抄録: We developed high functionality and quality (HFQ) lipids for facile and rapid preparation of ligand-grafted PEGylated liposomes.Because HFQ lipids are designed to exhibit good water dispersibility, ligand-grafted PEGylated liposomes can be easily prepared using the post-insertion method. The aim of this study is to develop novel VTWTPQAWFQWV (VTW) peptide-HFQ lipid to target human glioma cells. In order to disperse in water, VTW-(SG)5-lipid derivatives containing various amino acid residues with different charges were synthesized. Based on our previous work, (SG)5, a serine-glycine repeated peptide with a discrete molecular weight, was used as a spacer between the VTW and lipid. Of the derivatives tested, VTW-K3-(SG)5-lipid with three lysine residues showed the highest dispersibility in water,and VTW-K3-(SG)5/PEGylated liposomes can be prepared using the post-insertion method. The sizes of PEGylated liposomes and VTW-K3-(SG)5/PEGylated liposomes were 69.5 ± 4.4 and 74.4 ± 5.0 nm, respectively.In addition, the zeta potentials of PEGylated liposomes and VTW-K3-(SG)5/PEGylated liposomes were −2.7 ± 1.6 and −1.3 ± 0.3 mV, respectively. We found that VTW-K3-(SG)5/PEGylated liposomes selectively associated with human glioma U251MG cells.We succeeded in developing water-dispersible VTW-K3-(SG)5-lipids for the preparation of VTW-grafted PEGylated liposomes for glioma cell targeting.
キーワード: liposomes / targeting / PEG / hydrophobic peptide / glioma
URI: http://hdl.handle.net/10069/38803
ISSN: 17732247
DOI: 10.1016/j.jddst.2018.12.037
権利: ©2019 Elsevier. 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/10069/38803

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