Formulation of highly soluble poly(ethylene glycol)-peptide DNA condensates
摘要:
Two poly(ethylene glycol) (PEG)-peptides were synthesized and tested for their ability to bind to plasmid DNA and form soluble DNA condensates with reduced spontaneous gene expression. PEG-vinyl sulfone or PEG-orthopyridyl disulfide were reacted with the sulfhydryl of Cys-Trp-Lys<sub>18</sub> (CWK<sub>18</sub>) resulting in the formation of nonreducible (PEG-VS-CWK<sub>18</sub>) and reducible (PEG-SS-CWK<sub>18</sub>) PEG- peptides. Both PEG-peptides were prepared on a micromole scale, purified by RP-HPLC in >80% yield, and characterized by 1H NMR and MALDI-TOF. PEG-peptides bound to plasmid DNA with an apparent affinity that was equivalent to alkylated (Alk)CWK<sub>18</sub>, resulting in DNA condensates with a mean diameter of 80–90 nm and Z (zeta) potential of +10 mV. The particle size of PEG-peptide DNA condensates was constant throughout the DNA concentration range of 0.05–2 mg/mL, indicating these to be approximately 20-fold more soluble than AlkCWK<sub>18</sub> DNA
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DOI:
10.1021/js990072s
被引量:
年份:
1999
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