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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概要
- 論文の詳細を見る
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.
- ELSEVIER SCIENCE BVの論文
- 2010-08-30
著者
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原島 秀吉
北大院・薬学研究科
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SHIGENOBU Kohki
Faculty of Pharmaceutical Sciences, University of Tokyo
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Harashima Hideyoshi
Department Of Pharmacokinetics And Pharmaceutics Graduate School Of Pharmaceutical Sciences The Univ
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Hida Kyoko
Department Of Vascular Biology Hokkaido University Graduate School Of Dental Medicine
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Ohga Noritaka
Department Of Vascular Biology Hokkaido University Graduate School Of Dental Medicine
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Hida Kyoko
Department Of Oral Pathology And Biology Division Of Vascular Biology Hokkaido University
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Harashima Hideyoshi
Fac. Of Pharmaceutical Sciences Hokkaido Univ. Kita-12 Nishi-6 Kita-ku Sapporo 060-0812 Jpn
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