Design of a dual-ligand system using a specific ligand and cell penetrating peptide, resulting in a synergistic effect on selectivity and cellular uptake

Takara, Kazuhiro; Hatakeyama, Hiroto; Ohga, Noritaka; Hida, Kyoko; Harashima, Hideyoshi

Design of a dual-ligand system using a specific ligand and cell penetrating peptide, resulting in a synergistic effect on selectivity and cellular uptake

Takara, Kazuhiro; Hatakeyama, Hiroto; Ohga, Noritaka et al.

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2010, 396(1-2), 143-148

Permalink : https://hdl.handle.net/2115/46736

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アクセス権	open access
URI	https://hdl.handle.net/2115/46736
タイトル	Design of a dual-ligand system using a specific ligand and cell penetrating peptide, resulting in a synergistic effect on selectivity and cellular uptake
著者	Takara, Kazuhiro ; Hatakeyama, Hiroto ; Ohga, Noritaka ; Hida, Kyoko ; Harashima, Hideyoshi
著者名 Takara, Kazuhiro
e-Rad_Researcher 70504786 著者名 Hatakeyama, Hiroto
著者名 Ohga, Noritaka
著者名 Hida, Kyoko
著者名 Harashima, Hideyoshi
言語	英語
キーワード	Dual-ligand
	Active targeting
	Cell penetrating peptide
	NGR
	Tumor endothelial cells
発行日	2010-08-30
出版者	ELSEVIER SCIENCE BV
収録物名	INTERNATIONAL JOURNAL OF PHARMACEUTICS
巻(号)	396(1-2)
ページ	143-148
抄録	In this study, a dual-ligand liposomal system comprised of a specific ligand and a cell penetrating peptide (CPP) is described to enhance selectivity and cellular uptake. Dual-ligand PEGylated liposomes were prepared by modifying the end of the PEG with an NGR motif peptide, followed by a surface coating of the liposomes with stearylated oligoarginine (STR-RX) The NGR motif recognizes CD13. a marker protein located on tumor endothelial cells A suitable number of RX units was determined to be R4, since it can be masked by the PEG aqueous layer Although no enhanced cellular uptake was observed when a single modification of PEGylated liposomes with either NGR- or STR-R4 was used, the dual-modification with NGR and STR-R4 stimulated uptake of PEGylated liposomes by CD13 positive cells, and this uptake was superior to that obtained by PEG-unmodified liposomes modified with STR-R4 The dual-ligand system shows a synergistic effect on cellular uptake Collectively, the dual-ligand system promises to be useful in the development efficient and specific drug delivery systems. (C) 2010 Elsevier B V All rights reserved.
資源タイプ	学術雑誌論文
出版タイプ	Accepted Manuscript
PISSN	0378-5173
関連情報	PMID 20457236
関連情報 (isVersionOf)	出版社版DOI https://doi.org/10.1016/j.ijpharm.2010.05.002