Targeted Charge-Reversal Nanoparticles for Nuclear Drug Delivery

Department of Animal Science, University of Wyoming, Ларами, Wyoming, United States
Angewandte Chemie International Edition (Impact Factor: 11.26). 06/2007; 46(26):4999-5002. DOI: 10.1002/anie.200605254
Source: PubMed


(Figure Presented) Reversing the charges: Targeted charge-reversal nanoparticles (TCRNs) comprised of poly(ε-caprolactone)-block- polyethyleneimine (PCL-PEI), whose amine groups are converted into amides, are negatively charged at neutral pH but become positively charged at pH < 6 (see picture). TCRNs effectively enter cells, regenerate the PEI layer in lysosomes, and localize in the nucleus for nuclear drug delivery.

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    • "Amide linkage conjugated with a carbon–carbon double bond in position has been confirmed as an acid-cleavable bond due to intramolecular self-catalysis of carboxyl, which was commonly used in charge-reversal gene delivery systems [54] [55] [56]. Neuropilin- 1 (Nrp-1) is a transmembrane receptor glycoprotein which plays a predominant role in angiogenesis and vascular permeability. "
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