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


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 1H and 13C 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.

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Rasolonjatovo, B. , Pitard, B. , Guégan, P. and Cheradame, H. (2014) An Overview of the Synthesis and Gene Transfer Properties of Triblock Copolymers Poly(2-Methyl-2-Oxazoline-b-Tetrahydrofurane-b-2-Methyl-2-Oxazoline). Journal of Biomaterials and Nanobiotechnology, 5, 53-65. doi: 10.4236/jbnb.2014.52008.

Conflicts of Interest

The authors declare no conflicts of interest.


[1] Xia, G. and Leaf, H. (2012) Recent Advances in Nonviral Vectors for Gene Delivery. Accounts of Chemical Research, 45, 971-979.
[2] Meredith, A.M. and Eric, E.S. (2009) Nonviral Vectors for Gene Delivery. Chemical Reviews, 109, 259-302.
[3] Toussignant, J.D., Gates, A.L., Ingram, L.A., Johnson, C.L., Nietupski, J.B., Cheng, S.H., Eastman, S.J. and Scheule, R.K. (2000) Comprehensive Analysis of the Acute Toxicity Induced by Systemic Administration of Cationic Lipid:Plasmid:DNA Complexes in Mice. Human Gene Therapy, 11, 2493-2513.
[4] Brissault, B., Leborgne, C., Guis, C., Danos, O., Cheradame, H. and Kichler, A. (2006) Linear Topology Confers in Vivo Gene Transfer Activity to Polyethylenimines. Bioconjugate Chemistry, 17, 759-765.
[5] Cheradame, H., Brissault, B., Guis, C., Guégan, P., Pomel, C., Kichler, A., Gau, J. and Auvray, L. (2006) Improvement of Synthetic Vectors for Gene Therapy Using Ring-Opening Cationic Polymerization. Macromolecular Symposia, 240, 166-177.
[6] Brissault, B., Kichler, A., Leborgne, C., Danos, O., Cheradame, H., Gau, J., Auvray, L. and Guis, C. (2006) Synthesis, Characterization, and Gene Transfer Application of Poly(ethylene glycol-b-ethylenimine) with High Molar Mass Polyamine Block. Biomacromolecules, 7, 2863-2870.
[7] Behr, J.P. (2012) Synthetic Gene Transfer Vectors II: Back to the Future. Accounts of Chemical Research, 45, 980-984.
[8] Bromberg, L., Alakhov, V.Y. and Hatton, T.A. (2006) Self-Assembling Pluronic-Modified Polycations in Gene Delivery. Current Opinion in Colloid and Interface Science, 11, 217-223.
[9] Pitard, B., Pollard, H., Agbulut, O., Lambert, O., Vilquin, J.T., Cherel, Y., Abadie, J., Samuel, J.L., Rigaud, J.L., Menoret, S., Anegon, I. and Escande, D. (2002) Nonionic Amphiphile Agent Promotes Gene Delivery in Vivo to Skeletal and Cardiac Muscles. Human Gene Therapy, 13, 1767-1775.
[10] Merdan, T., Kopecek, J. and Kissel, T. (2002) Prospects for Cationic Polymers in Gene and Oligonucleotide Therapy against Cancer. Advanced Drug Delivery Reviews, 54, 715-758.
[11] De Witte, I.C. and Goethals, E.J. (1999) Synthesis and Block Specific Complexation of Poly(ethylene oxide)-poly(tetrahydrofuran)-poly(ethylene oxide) Triblock Copolymers. Polymers for Advanced Technologies, 10, 287-292.<287::AID-PAT877>3.0.CO;2-F
[12] Cheradame, H., Pomel, C., Sassatelli, M., Sanh, A., Gau, J., Bacri, L., Auvray, L. and Guégan, P. (2008) Tuning Macromolecular Structure of Synthetic Vectors for Gene Therapy. Macromolecular Symposia, 261, 167-181.
[13] Pitard, B., Bello-roufai, M., Lambert, O., Richard, P., Desigaux, L., Fernandes, S., Lanctin, C., Pollard, H., Eeghal, M., Rescan, P.Y. and Escande, D. (2004) Negatively Charged Self-Assembling DNA/Poloxamine Nanospheres for in Vivo Gene Transfer. Nucleic Acids Research, 32, e159.

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