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-polystyrenen(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 H-1 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 NAC-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. (C) 2015 Elsevier B.V. All rights reserved.