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-polystyrene130 (P(St-alt-MA)58-b-PSt130) 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-PSt130) was characterized by FTIR and (1)H NMR. The NAG-P(St-alt-MA)58-b-PSt130 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-PSt130 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-PSt130 nanoparticles. Anticancer activity toward MCF-7 cells and HT29 cells showed that DOX-loaded NAG-P(St-alt-MA)58-b-PSt130 nanoparticles exhibited a higher antitumor activity compared to DOX-loaded P(St-alt-MA)58-b-PSt130 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-PSt130 nanoparticles may be used as an effective targeting drug delivery system for cancer therapy.
School of Pharmacy, Binzhou Medical University, Yantai, PR China.
Baocheng
B
Tian
School of Pharmacy, Binzhou Medical University, Yantai, PR China.
Yuanyuan
Y
Ding
School of Pharmacy, Binzhou Medical University, Yantai, PR China; Argenta Limited, PO Box 75 340, Manurewa 2102, Auckland, New Zealand.
Jian
J
Han
School of Pharmacy, Binzhou Medical University, Yantai, PR China.
Jing
J
Zhang
Department of Pathology, Binzhou Medical University Hospital, Binzhou, PR China.
Yuzhen
Y
Han
School of Pharmacy, Binzhou Medical University, Yantai, PR China. Electronic address: hanjingtian002@163.com.
Jingtian
J
Han
D000117:Acetylglucosamine / Q000737:chemistry*; D000903:Antibiotics, Antineoplastic / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D019073:HT29 Cells; D006801:Humans; D061986:MCF-7 Cells; D018613:Microscopy, Confocal; D046529:Microscopy, Electron, Transmission; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011108:Polymers / Q000737:chemistry*; D017550:Spectroscopy, Fourier Transform Infrared
D000903:Antibiotics, Antineoplastic; D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D011108:Polymers; D004317:Doxorubicin; D000117:Acetylglucosamine
Cancer targeting; Drug delivery; N-acetyl glucosamine; Nanoparticles