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  • Linear polyethyleneimine grafted to a hyperbranched poly(ethylene glycol)-like core: a copolymer for gene delivery.

Linear polyethyleneimine grafted to a hyperbranched poly(ethylene glycol)-like core: a copolymer for gene delivery.

Bioconjugate chemistry (2006-01-19)
Pallab Banerjee, Ralph Weissleder, Alexei Bogdanov
ABSTRACT

A block copolymer of a hyperbranched poly(ethylene glycol)-like core and linear polyethylenimine (HBP) was synthesized by a facile synthetic route that included (1) a single-step cationic copolymerization of diepoxy and polyhydroxyl monomers, (2) derivatization of hydroxyl groups of the core HBPEG copolymer with either tosyl or chloromethylbenzoyl chlorides resulting in a corresponding macroinitiator, and (3) synthesis of HBPEG-block-poly(alkyl oxazolines). HBPEG-block-linear polyethyleneimine (HBP) was obtained by hydrolysis of HBPEG-block-poly(alkyl oxazolines). Linear PEI-bearing hyperbranched polycations (HBP) had lower inherent toxicity in cell culture than PEG-grafted linear polyethyleneimines (PEGLPEI). PEGLPEI formed a complex with DNA with an average diameter of 250 nm. The complexes were loosely condensed and formed aggregates and precipitates during storage. By contrast, hyperbranched polycations (HBP) formed approximately 50 nm nanocomplexes with DNA that were stable for several weeks and showed resistance to DNAse I-mediated degradation. The 'inverted' block copolymers showed several orders of magnitude higher transfection efficiency than PEGLPEI in vitro. Because of the biocompatibility and higher transfection efficiency, the 'inverted' block copolymer merits further investigation as a gene carrier.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Linear polyethylenimine-block-poly(ethylene glycol), PEG average Mn 5,000, PEI average Mn 5,000
Sigma-Aldrich
Linear polyethylenimine-block-poly(ethylene glycol), PEG average Mn 5,000, PEI average Mn 10,000
Sigma-Aldrich
Linear polyethylenimine-block-poly(ethylene glycol), PEG average Mn 5,000, PEI average Mn 30,000
Sigma-Aldrich
Linear polyethylenimine-block-poly(ethylene glycol), PEG average Mn 2,000, PEI average Mn 20,000
Sigma-Aldrich
Linear polyethylenimine-block-poly(ethylene glycol), PEG average Mn 2,000, PEI average Mn 30,000
Sigma-Aldrich
Linear polyethylenimine-block-poly(ethylene glycol), PEG average Mn 2,000, PEI average Mn 10,000
Sigma-Aldrich
Linear polyethylenimine-block-poly(ethylene glycol), PEG average Mn 750, PEI average Mn 15,000
Sigma-Aldrich
Linear polyethylenimine-block-poly(ethylene glycol), PEG average Mn 750, PEI average Mn 10,000
Sigma-Aldrich
Linear polyethyleneimine-block-poly(ethylene glycol), PEG average Mn 5000, PEI average Mn 20000
Sigma-Aldrich
Poly(ethylene glycol)-block-polyethyleneimine, PEG Mn 750, PEI Mn 15k