N-acetyl-d-glucosamine decorated polymeric nanoparticles for targeted delivery of doxorubicin: Synthesis, characterization and in vitro evaluation

A novel targeting drug delivery system containing poly(styrene-alt-maleic anhydride) 58 -b-polystyrene 130 (P(St-alt-MA) 58 -b-PSt 130 ) as a copolymer backbone, N -acetyl glucosamine (NAG) as a targeting moiety was designed and synthesized. The NAG grafted copolymer (NAG-P(St-alt-MA) 58 -b-PSt 130 ) was characterized by FTIR and 1 H NMR. The NAG-P(St-alt-MA) 58 -b-PSt 130 nanoparticles exhibited spherical shapes with an average diameter about 56.27   ±   0.43   nm, low critical micelle concentration of 0.028   mg/mL, negative zeta potential −41.46   ±   0.99   mV, high drug loading 25.83   ±   1.09% and encapsulation efficiency 69.69   ±   3.98%. In vitro cell cytotoxicity was conducted to confirm the safety of the NAG-P(St-alt-MA) 58 -b-PSt 130 nanoparticles. Confocal laser scanning microscopy (CLSM) and flow cytometry (FCM) results showed that the NAG targeting moiety enhanced the internalization and targeting ability of NAG-P(St-alt-MA) 58 -b-PSt 130 nanoparticles. Anticancer activity toward MCF-7 cells and HT29 cells showed that DOX-loaded NAG-P(St-alt-MA) 58 -b-PSt 130 nanoparticles exhibited a higher antitumor activity compared to DOX-loaded P(St-alt-MA) 58 -b-PSt 130 nanoparticles, which could attribute to NAG receptor-mediated endocytosis. These results suggest that the biocompatible and non-toxic NAG-P(St-alt-MA) 58 -b-PSt 130 nanoparticles may be used as an effective targeting drug delivery system for cancer therapy.