Substantial research is marked in the field of cationic polymers and their derivatives as gene delivery vectors and even resulted in clinical trials. Hydrophobic modi?cations proved to be a promising approach to improve the ef?ciency of cationic polymeric gene delivery vectors. A small library of aminoglycoside based polymers were synthesized by taking aminoglycoside as the monomers and the glycerol diglycidyl ether as the linker group. Their transfection profiles were evaluated in different types of cancer cells and proved to be more efficient than the standard poly(ethylene imine). With a view to further enhance the transfection profiles of the lead polymers, lipids of varying chain length were conjugated to the polymers by N-acylation. The conjugates synthesized were well characterized using 1H NMR and FTIR spectroscopy. Screening of lipid-conjugated polymers in different cancer cells for evaluation of transfection profiles led to identification of some leads, which showed superior transfection profiles when compared to the parent polymers and poly (ethylene imine). Structure-Activity Investigation revealed that the transfection profiles depends on several factors such as the type of cell line, the kind of polymer, the kind of lipid used for modification, and the degree of conjugation. The influence of the various physicochemical properties including polyplex size, zeta potential, and DNA binding on transgene expression efficacies were also investigated. A characteristic feature of this study is that some of the leads proved to be serum compatible. Taken together, these materials show significant promise in non-viral transgene delivery, and may be attractive for gene therapy applications.

Synthesis and in vitro transfection studies of lipid modified polymers: A structure- activity investigation

247th National Meeting (2014)

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