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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
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)
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Submitter: 畠山 浩人
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