Preparation of Pluronic Grafted Dendritic alpha,epsilon-poly(L-lysine)s and Characterization as a Delivery Adjuvant of Antisense Oligonucleotide.

A series of pluronic grafted dendritic alpha,epsilon-poly(L-lysine)s (DPL-PF127) were synthesized by a conjugation reaction and evaluated the potential use of DPL-PF127 as a delivery agent of antisense oligonucleotide into A375 B3 cells. The structural features of the DPL-PF127 were identified by NMR and FT-IR. The number of pluronic F127 on DPL surface, determined by fluorescamine assay, increased proportionally to the mole ratio between DPL and activated PF127 in reaction. DPL- PF127 showed the physical properties of decrease in zetapotential and increase in size as the mole ratio of PF127 to DPL increased. The complex formation of DPL-PF127 with oligonucleotide was confirmed by running capillary zone electrophoresis (CZE) and agarose gel electrophoresis. DPL-PF127, prepared at the mole ratio of 1:10 in reaction, was the most suitable as a delivery adjuvant of oligonucleotide. In addition, DPL-PF127/oligonucleotide complexes were taken into A375B3 cell without cellular toxicity and delivered antisense oligonucleotide into cell.