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

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.

収録刊行物

• INTERNATIONAL JOURNAL OF PHARMACEUTICS

  INTERNATIONAL JOURNAL OF PHARMACEUTICS 396 (1-2), 143-148, 2010-08-30

  ELSEVIER SCIENCE BV

キーワード

• Dual-ligand
• Active targeting
• Cell penetrating peptide
• NGR
• Tumor endothelial cells

詳細情報

• CRID: 1050564288960381568
• NII論文ID: 120003118155
• HANDLE: 2115/46736
• ISSN: 03785173
• 本文言語コード: en
• 資料種別: journal article
• データソース種別:
  • IRDB
  • CiNii Articles