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

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Please use this identifier to cite or link to this item:http://hdl.handle.net/2115/46736

Title: Design of a dual-ligand system using a specific ligand and cell penetrating peptide, resulting in a synergistic effect on selectivity and cellular uptake
Authors: Takara, Kazuhiro Browse this author
Hatakeyama, Hiroto Browse this author →KAKEN DB
Ohga, Noritaka Browse this author
Hida, Kyoko Browse this author
Harashima, Hideyoshi Browse this author
Keywords: Dual-ligand
Active targeting
Cell penetrating peptide
NGR
Tumor endothelial cells
Issue Date: 30-Aug-2010
Publisher: ELSEVIER SCIENCE BV
Journal Title: INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume: 396
Issue: 1-2
Start Page: 143
End Page: 148
Publisher DOI: 10.1016/j.ijpharm.2010.05.002
PMID: 20457236
Abstract: 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.
Type: article (author version)
URI: http://hdl.handle.net/2115/46736
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 畠山 浩人

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