title: Bioreducible heparin-based nanogel drug delivery system.
abstract: Bioreducible heparin (HEP)-based nanogels were prepared by derivatizing HEP with vinyl group followed by copolymerizing with cystamine bisacrylamide in aqueous medium in the absence of surfactant. The hydrodynamic diameter of the HEP nanogels could be tuned in the range from 80 to 200 nm. Doxorubicin (DOX) was loaded into the HEP nanogels, and high drug loading content (30%) and efficiency (90%) were achieved. In vitro drug release test revealed that this drug delivery system exhibited strongly redox-sensitive drug release behavior that would greatly favor the in vivo drug delivery performance of the nanogels. After injected into tumor-bearing mice through tail vein, the DOX-loaded HEP nanogels showed remarkable accumulation in tumors as demonstrated by in vivo near infared fluorescence imaging and ex vivo DOX concentration measurements. The doxorubicin accumulation at tumor site goes beyond 9% injected dose per gram of tumor through such delivery system, making that DOX-loaded HEP nanogels have significantly superior in vivo antitumor activity.
authors.affiliation: Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Wu
authors.affiliation: Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Yao
authors.affiliation: Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, PR China.
authors.forename: Xin
authors.initials: X
authors.lastname: Wang
authors.affiliation: Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, PR China.
authors.forename: Chen
authors.initials: C
authors.lastname: Xie
authors.affiliation: Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, PR China.
authors.forename: Jialiang
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Department of Polymer Science & Engineering, College of Chemistry & Chemical Engineering, Nanjing University, Nanjing 210093, PR China. Electronic address: jiangx@nju.edu.cn.
authors.forename: Xiqun
authors.initials: X
authors.lastname: Jiang
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000737:chemistry* / Q000627:therapeutic use*; D016503:Drug Delivery Systems / Q000379:methods*; D006493:Heparin / Q000737:chemistry* / Q000627:therapeutic use*; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy; D008297:Male; D051379:Mice; D000080385:Nanogels; D011092:Polyethylene Glycols / Q000737:chemistry*; D011094:Polyethyleneimine / Q000737:chemistry*
chemical_list: D000080385:Nanogels; C052784:doxorubicin-heparin; C413692:polyethylene glycol polyethyleneimine nanogel; D011092:Polyethylene Glycols; D004317:Doxorubicin; D011094:Polyethyleneimine; D006493:Heparin
keywords: Antitumor; Doxorubicin; Heparin; Nanogel