An Overview of the Synthesis and Gene Transfer Properties of Triblock Copolymers Poly(2-Methyl-2-Oxazoline-b-Tetrahydrofurane-b-2-Methyl-2-Oxazoline)

Abstract

The synthesis of poly(2-methyl-2-oxazoline-b-tetrahydrofurane-b-2-methyl-2-oxazoline) triblock copolymer of low molar mass has been carried out. Characterization of the purified polymer by 1 H and 13 C NMR spectroscopies is described. These block copolymers did not give DNA containing polyplexes. The in vivo transfection properties were investigated by injection of tibialis muscles and intratracheal administration of female Swiss mice. These triblock copolymers with a molar ratio [2-methyl-2-oxazoline units]/[tetrahydrofurane units] in the 3 - 5 range gave a higher transfection efficiency than that of Lutrol or of PE6400 which are the gold standards of this transfection technique. Hydrolysis increased the performances of muscle transfection, showing the beneficial effect of the presence of positive charges, but was clearly detrimental to the transfection efficiency of pulmonary epithelium.