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Versatile hybrid polyethyleneimine–mesoporous carbon nanoparticles for targeted delivery

Wan, Long, Zhao, Qinfu, Zhao, Peng, He, Bing, Jiang, Tongying, Zhang, Qiang, Wang, Siling
Carbon 2014 v.79 pp. 123-134
antineoplastic activity, carbon nanoparticles, chemical bonding, confocal microscopy, drugs, flow cytometry, fluorescein, folate receptors, folic acid, growth retardation, image analysis, isothiocyanates, mice, neoplasm cells, neoplasms, pH, paclitaxel, polyethyleneimine, porous media
To meet the needs of targeted drug delivery and medical imaging, uniform mesoporous carbon spheres (UMCS) were functionalized using hyperbranched polyethyleneimine (PEI) covalently linked with fluorescein isothiocyanate (FITC) and folic acid (FA). Folate-receptor-positive KB cancer cells internalized five times more nanoparticles than A549 cells deficient in folate receptors in vitro using flow cytometry and confocal microscopy. The in vivo distribution results also confirmed that the FA–PEI–FITC–UMCS nanoparticles could target the FA-positive tumors. In addition, the specifically targeted hybrid carbon nanoparticles exhibited non-cytotoxic and controlled intracellular release (pH dependent) of the loaded agents. The in vivo antitumor effect of the paclitaxel (PTX)-loaded nanoparticles was investigated in Kunming mice harboring a hepatic H22 tumor. PTX-loaded FA–PEI–UMCS nanoparticles displayed superior antitumor effects compared to other PTX formulations, and the tumor growth inhibition rate was 86.53% compared with the control group (saline) for the enhanced targeted accumulation of NPs in tumor cells.