New pegylated polyaspartamide-based polyplexes as gene delivery vectors.
OBJECTIVE
To synthesize novel polyhydroxyethylaspartamide (PHEA) copolymers containing spermine (Spm) and polyethylene glycol (PEG) moieties in high yields, with the expectation that this material would show stealth properties and the ability to complex DNA by electrostatic interactions.


METHODS
PHEA-PEG-Spm copolymer was prepared with a two-step reaction. Chemical, physicochemical and biological characterizations of PHEA-PEG-Spm copolymers and their obtained polyplexes with pDNA were performed.


RESULTS
The introduction of spermine in PHEA structure allows to obtain a copolymer bearing in the side chains polyamine moieties capable to interact with DNA. On the other hand, the introduction of PEG in polymeric structure increased the DNA condensing ability of PHEA-PEG-Spm copolymer in comparison with the derivatives without PEG (PHEA-Spm), and improved its characteristics of biocompatibility.


CONCLUSIONS
PHEA-PEG-Spm copolymer shows excellent ability to complex and condense plasmidic DNA giving interpolyelectrolyte complexes to act as gene delivery systems. Moreover, PEGylation confers to the obtained interpolyelectrolyte complexes stealth properties.
Laboratory of Biocompatible Polymers, Department Chimicae Tecnologie Farmaceutiche, University of Palermo, Via Archirafi, 32, 90123 Palermo, Italy. gennacav@unipa.it
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Cavallaro
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Licciardi
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Scirè
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Di Stefano
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Giammona
D000818:Animals; D004247:DNA / Q000737:chemistry; D004573:Electrolytes; D004912:Erythrocytes / Q000187:drug effects; D018014:Gene Transfer Techniques; D005822:Genetic Vectors; D006801:Humans; D008546:Melanoma, Experimental; D051379:Mice; D008956:Models, Chemical; D036103:Nanotechnology / Q000379:methods*; D010455:Peptides / Q000737:chemistry*; D011073:Polyamines / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry*; D013096:Spermine / Q000737:chemistry; D055672:Static Electricity
D004573:Electrolytes; D010455:Peptides; D011073:Polyamines; C017645:polyaspartate; D013096:Spermine; D011092:Polyethylene Glycols; D004247:DNA