Effect of homobifunctional crosslinkers on nucleic acids delivery ability of PEI nanoparticles.

摘要: Abstract Polyethylenimine (PEI), a widely used cationic polymeric vector with high transfection efficiency, was converted into nanoparticles by introducing ionic and covalent crosslinkers varying proportion of 1,6-hexanebisphosphate (HP), adipic acid (AA) 1,4-butane dialdehyde (BA) to obtain small library HP-PEI (HPP), AA-PEI (AAP) BA-PEI (BAP) nanoparticles, respectively. Particles were characterized spectroscopic technique as well physicochemical parameters such size, morphology, surface charge, effect crosslinking on buffering capacity DNA binding ability. The entire series compared for their cytoxicity ability deliver genes in various cell lines. Among AAP-3 nanoparticle/DNA complex exhibited higher efficiency (1.5–7.8 folds) than the native PEI (25 kDa) commercially available reagents, GenePorter™, GenePorter2™, Fugene™ Superfect™, viability >85%. highest observed BAP (>95%). Importantly, activity complexes preserved presence serum. Transfection GFP-siRNA inhibited expression transfected GFP gene ∼81–92%. All nanoparticle types (HPP, AAP BAP) required comparable time entry cells subsequent intracellular passage from cytoplasm nucleus. Intravenous delivery 99 Tc labeled BAP-2/DNA female Balb/c mice revealed most organs retention liver. In conclusion, HPP, are safe efficient delivery.