Chitosan Grafted with Phosphorylcholine and Macrocyclic Polyamine as an Effective Gene Delivery Vector: Preparation, Characterization and In Vitro Transfection

Herein, an effective gene delivery vector phosphorylcholine and macrocyclic polyamine grafted chitosan (PC‐ g (6)‐Cs‐ g (2)‐Cyclen) was developed. Chemical characterization of product PC‐ g (6)‐Cs‐ g (2)‐Cyclen was performed by NMR, FT‐IR, gel permeation chromatography (GPC), and X‐ray photoelectron spectroscopy (XPS) analysis. PC‐ g (6)‐Cs‐ g (2)‐Cyclen could more efficiently bind and protect plasmid DNA than macrocyclic polyamine grafted chitosan (Cs‐ g ‐Cyclen) and phosphorylcholine grafted chitosan (Cs‐ g ‐PC), as evaluated by agarose gel electrophoresis, circular dichroism spectra, and fluorescence quenching assays. PC‐ g (6)‐Cs‐ g (2)‐Cyclen could wrap DNA into uniform nanoparticles in the size of 112.6 ± 8.5 nm and possessed net cationic charge. UV spectroscopy and MTT assays showed excellent water‐solubility and cell viability for PC‐ g (6)‐Cs‐ g (2)‐Cyclen. In addition, three polymer/DNA complexes showed 5.1−15.1‐fold greater uptake activity and 10−14‐fold higher transfection efficiency in 293 T cells as compared to chitosan/DNA complex, in which PC‐ g (6)‐Cs‐ g (2)‐Cyclen demonstrated the highest transfection activity. These date demonstrated that PC‐ g (6)‐Cs‐ g (2)‐Cyclen is a promising vector candidate for gene delivery.