A reduction-triggered delivery by a liposomal carrier possessing membrane-permeable ligands and a detachable coating

Takuro Maeda, Keiji Fujimoto

研究成果: Article査読

61 被引用数 (Scopus)

抄録

To control the cellular uptake of drugs and genes, we synthesized a liposomal carrier possessing membrane-permeable ligands and a detachable poly(ethylene glycol) (PEG) coating. For the detachable coating, a lipid having a thiolytic cleavable spacer (PEG-S-S-DOPE) was synthesized by the reaction of dioleoylphosphatidylethanolamine (DOPE) with a PEG chain via a disulfide linkage. The liposomes were prepared from a mixture of dipalmitoylphosphatidylcholine (DPPC), DOPE, PEG-S-S-DOPE, and cholesteryl hemisuccinate (CHEMS). The octamer (R8 peptide) of arginine was chosen as the membrane-permeable ligand and covalently immobilized onto the CHEMS portion of the liposome surface (PEG-S-S-R8-liposome). The disulfide bond of the PEG chain was cleaved to display the R8 peptides on the liposome surface by adding a reducing agent such as l-cysteine, and thereby internalization of the liposomes was significantly facilitated. When l-cysteine was added to the mixture of cells and the liposome that incorporated plasmids encoding the enhanced green fluorescence protein (pEGFP), the expression of EGFP was low but could be observed in almost 100% of the cells.

本文言語English
ページ(範囲)15-21
ページ数7
ジャーナルColloids and Surfaces B: Biointerfaces
49
1
DOI
出版ステータスPublished - 2006 4 15

ASJC Scopus subject areas

  • バイオテクノロジー
  • 表面および界面
  • 物理化学および理論化学
  • コロイド化学および表面化学

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