Investigation of the Oligonucleotide Nanosize Delivery System with the Function of Targeting to Tumor Cells

The effects of the tested factors including pH value, NaCl concentration, ODN concentration and charge ratio on the size and zeta potentials of nanoparticles (ODN-PLL, PLL: poly(l-lysine)s) were investigated by use of uniform design and NGR peptides were used to modify the nanoparticles, indicating that none of the tested factors was correlated with nanoparticles' size, however, a linear correlation (r = 0.8505) was found between charge ratio and zeta potential. A nanosize delivery system (ODN-PLL-NGR) with the function of targeting to tumor cells was developed by use of PLL to condense oligonucleotide into nanoparticles coated with peptide containing NGR motif. The ODN-PLL-NGR had the ability to protect ODN against nuclease degradation, and its cell uptake increased with time increment after incubation at 37°C for 40, 50 and 60 min.