Self-aggregates of oligoarginine-conjugated poly(amino acid) derivatives as a carrier for intracellular drug delivery

Biotechnol Lett. 2005 Jul;27(14):977-82. doi: 10.1007/s10529-005-7838-4.

Abstract

N(omega)-2,2,4,6,7-Pentamethyldihydrobenzofuran-5-sulfonyl (N(omega)-Pbf)-protected oligoarginine was directly conjugated to poly(amino acid) derivatives modified with a long alkyl chain. The final concentration of conjugated peptides was easily controlled by the feed ratio of oligoarginine to polymer backbone and a final soluble polymeric system was obtained by the deprotection of N(omega)-Pbf groups. The polymeric conjugates formed stable self-aggregates of size range of 8-40 nm in aqueous solution and effectively internalized into HeLa cells by adsorptive endocytosis.

MeSH terms

  • Drug Delivery Systems*
  • Endocytosis* / drug effects
  • HeLa Cells
  • Humans
  • Peptides / chemistry
  • Peptides / pharmacology*

Substances

  • Peptides
  • polyarginine