Journal
JOURNAL OF BIOMEDICAL MATERIALS RESEARCH PART A
Volume 86A, Issue 1, Pages 137-148Publisher
WILEY
DOI: 10.1002/jbm.a.31331
Keywords
intracellular delivery; polymer-peptide conjugate; oligoarginine; poly(amino acid)s; synthetic delivery carrier
Funding
- National Research Foundation of Korea [과C6A1907, 2002-02845] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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Poly(2-hydroxytethyl aspartamide) (PHEA) was effectively translocated in both fixed and unfixed HeLa cells, when oligoarginine (Arg(8)) known as one of the cell-penetrating peptides was conjugated via a thioether linkage. The internalization of PHEA-Arg(8) into cells was a temperature-dependent process, and the studies at endocytosis inhibition conditions suggested that an endocytosis was a key mechanism. The fluorescence spectra of PHEA-Arg(8) in liposome solutions showed that PHEA-Arg(8) was collectively adsorbed in the negative liposome membrane due to the high cationic property of a conjugated Arg(8), representing that a surface adsorption was a first step in the internalization of PHEA-Arg(8). The membrane leakage activity of PHEA-Arg(8) was much tower than that of Arg(8) own, meaning that PHEA-Arg(8) does not effectively disrupt the cell membrane integrity. The uptake of polymer conjugates increased with the incubation time and reached saturation after several hours. The increase in the number of peptide conjugated to one polymer chain could increase the collective adsorption of polymer conjugates and enhance the cellular uptake. Thus, it is believed that PHEA-Arg(8) could be internalized by an adsorptive-endocytosis. A model conjugate of PHEA-Args with methotrexate (PHEA-MTX-Arg(8)) inhibited the cell proliferation about several orders of magnitude more active than PHEA-MTX. (C) 2007 Wiley Periodicals, Inc.
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