Intracellular delivery enhancement of poly(amino acid) drug carriers by oligoarginine conjugation.
作者： Seung Rim Yang , Seung Beom Kim , Cheol O. Joe , Jong-Duk Kim
DOI: 10.1002/JBM.A.31331
关键词:
摘要: Poly(2-hydroxytethyl aspartamide) (PHEA) was effectively translocated in both fixed and unfixed HeLa cells, when oligoarginine (Arg8) known as one of the cell-penetrating peptides conjugated via a thioether linkage. The internalization PHEA-Arg8 into cells temperature-dependent process, studies at endocytosis inhibition conditions suggested that an key mechanism. fluorescence spectra liposome solutions showed collectively adsorbed negative membrane due to high cationic property Arg8, representing surface adsorption first step PHEA-Arg8. leakage activity much lower than Arg8 own, meaning does not disrupt cell integrity. uptake polymer con&n132;jugates increased with incubation time reached saturation after several hours. increase number &n132;peptide chain could collective conjugates enhance cellular uptake. Thus, it is believed be internalized by adsorptive-endocytosis. A model conjugate methotrexate (PHEA-MTX-Arg8) inhibited proliferation about orders magnitude more active PHEA-MTX. © 2007 Wiley Periodicals, Inc. J Biomed Mater Res, 2008
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