Dual-ligand modification of PEGylated liposomes shows better cell selectivity and efficient gene delivery

Kibria, Golam; Hatakeyama, Hiroto; Ohga, Noritaka; Hida, Kyoko; Harashima, Hideyoshi

Dual-ligand modification of PEGylated liposomes shows better cell selectivity and efficient gene delivery

Kibria, Golam; Hatakeyama, Hiroto; Ohga, Noritaka et al.

Journal of Controlled Release, 2011, 153(2), 141-148

Permalink : https://hdl.handle.net/2115/47916

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アクセス権	open access
URI	https://hdl.handle.net/2115/47916
タイトル	Dual-ligand modification of PEGylated liposomes shows better cell selectivity and efficient gene delivery
著者	Kibria, Golam ; Hatakeyama, Hiroto ; Ohga, Noritaka ; Hida, Kyoko ; Harashima, Hideyoshi
著者名 Kibria, Golam
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	Targeted delivery
	Dual-ligand
	PEGylated liposome
	RGD motif
	Cell penetrating peptide
	Gene expression
発行日	2011-07-30
出版者	Elsevier
収録物名	Journal of Controlled Release
巻(号)	153(2)
ページ	141-148
抄録	The objective of this study was to develop an efficient dual-ligand based PEGylated liposomal delivery system that had target specificity as well as properties that would enhance cellular uptake. PEGylated liposomes (PEG-LP) were prepared by the lipid film hydration method by adding distearoyl phosphoethanolamine-polyethylene-glycol-2000 conjugate (DSPE-PEG2000) to a lipid mixture. The cyclic RGD (Arg-Gly-Asp) peptide, a specific ligand with affinity for Integrin αvβ3 was coupled to the distal end of the PEG on the PEG-LP (RGD-PEG-LP). Stearylated octaarginine (STR-R8) was incorporated on the surface of the RGD-PEG-LP as dual-ligand (R8/RGD-PEG-LP) that functions as a cell penetrating peptide (CPP). RGD-PEG-LP and R8/RGD-PEG-LP were preferentially taken up by caveolae-mediated and clathrin-mediated endocytosis pathways, respectively. Compared to PEG-LP, R8/RGD-PEG-LP showed an enhanced cellular uptake as well as a higher transfection efficiency in Integrin αvβ3 expressing cells. However, the amount of cellular uptake or gene expression by the single ligand versions was negligible, even in Integrin αvβ3 expressing cells. No remarkable difference in cellular uptake or gene expression was observed for cells in which the expression of targeted receptors was absent. It can be concluded that dual-ligand modified PEG-LP possesses a strong capability for the efficient internalization of PEG-LP and consequently would be an effective tool for the targeted delivery of macromolecules or chemotherapeutics through accelerated cellular uptake.
資源タイプ	学術雑誌論文
出版タイプ	Accepted Manuscript
PISSN	0168-3659
関連情報	PMID 21447361
関連情報 (isVersionOf)	出版社版DOI https://doi.org/10.1016/j.jconrel.2011.03.012