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Cited by 161

The DOI matches its Crossref record; 1 of the 1 references it cites were found in a registry or an index.

Novel Intracellular Delivery System of Antisense Oligonucleotide by Self-Assembled Hybrid Micelles Composed of DNA/PEG Conjugate and Cationic Fusogenic Peptide

Jeong, Ji Hoon, Kim, Sung Wan, Park, Tae Gwan·2003·Bioconjugate Chemistry

Abstract

An antisense oligonucleotide (ODN), c-myb, was covalently conjugated to poly(ethylene glycol) (PEG) via an acid-cleavable phosphoramidate linkage to form a diblock copolymer-like structure. The phosphoramidate linkage between ODN and PEG was completely cleaved within 5 h in an endosomal acidic condition (pH 4.7). When complexed with a cationic fusogenic peptide, KALA, the ODN/PEG conjugate self-associated to form polyelectrolyte complex micelles in an aqueous solution. The anionic ODN segments were ionically interacted with cationic KALA peptide to form an inner polyelectrolyte complex core, while the PEG segments constituted a surrounding corona. Effective hydrodynamic volume of the micelles was ca. 70 nm with a very narrow size distribution. The polyelectrolyte complex micelles, composed of c-myb ODN-PEG conjugate and KALA, were transported into cells far more efficiently than c-myb ODN itself. They also exhibited higher antiproliferative activity against smooth muscle cells. This study demonstrates that the DNA/PEG hybrid micelles system can be applied for the delivery of antisense oligonucleotide.

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Metadata

Authors
Jeong, J. H., Kim, S. W., & Park, T. G.
Venue
Bioconjugate Chemistry
Published
2003-03-01
Volume
14
Issue
2
Pages
473-479
ISSN
  • 1043-1802 (ISSN-L)
  • 1520-4812
OpenAlex
W2082293230
Cited by
161
References
1
FWCI
3.54
Type
journal article
Language
en
Open access
closed

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