title: GX1-conjugated poly(lactic acid) nanoparticles encapsulating Endostar for improved in vivo anticolorectal cancer treatment.
abstract: Tumor angiogenesis plays a key role in tumor growth and metastasis; thus, targeting tumor-associated angiogenesis is an important goal in cancer therapy. However, the efficient delivery of drugs to tumors remains a key issue in antiangiogenesis therapy. GX1, a peptide identified by phage-display technology, is a novel tumor vasculature endothelium-specific ligand and possesses great potential as a targeted vector and antiangiogenic agent in the diagnosis and treatment of human cancers. Endostar, a novel recombinant human endostatin, has been shown to inhibit tumor angiogenesis. In this study, we developed a theranostic agent composed of GX1-conjugated poly(lactic acid) nanoparticles encapsulating Endostar (GPENs) and labeled with the near-infrared dye IRDye 800CW to improve colorectal tumor targeting and treatment efficacy in vivo. The in vivo fluorescence molecular imaging data showed that GPENs (IRDye 800CW) more specifically targeted tumors than free IRDye 800CW in colorectal tumor-bearing mice. Moreover, the antitumor efficacy was evaluated by bioluminescence imaging and immunohistology, revealing that GPENs possessed improved antitumor efficacy on subcutaneous colorectal xenografts compared to other treatment groups. Thus, our study showed that GPENs, a novel GX1 peptide guided form of nanoscale Endostar, can be used as a theranostic agent to facilitate more efficient targeted therapy and enable real-time monitoring of therapeutic efficacy in vivo.
authors.affiliation: Key laboratory of Molecular Imaging, The state Key Laboratory of Management and Control for Complex Systems, Institute of Automation, Chinese Academy of Sciences, Beijing, People's Republic of China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Du
authors.affiliation: Key laboratory of Molecular Imaging, The state Key Laboratory of Management and Control for Complex Systems, Institute of Automation, Chinese Academy of Sciences, Beijing, People's Republic of China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Zhang
authors.affiliation: Department of Biomedical Engineering, College of Engineering, Peking University, Beijing People's Republic of China.
authors.forename: Lijia
authors.initials: L
authors.lastname: Jing
authors.affiliation: Department of Biomedical Engineering, College of Engineering, Peking University, Beijing People's Republic of China.
authors.forename: Xiaolong
authors.initials: X
authors.lastname: Liang
authors.affiliation: Key laboratory of Molecular Imaging, The state Key Laboratory of Management and Control for Complex Systems, Institute of Automation, Chinese Academy of Sciences, Beijing, People's Republic of China.
authors.forename: Chongwei
authors.initials: C
authors.lastname: Chi
authors.affiliation: Key laboratory of Molecular Imaging, The state Key Laboratory of Management and Control for Complex Systems, Institute of Automation, Chinese Academy of Sciences, Beijing, People's Republic of China.
authors.forename: Yaqian
authors.initials: Y
authors.lastname: Li
authors.affiliation: Key laboratory of Molecular Imaging, The state Key Laboratory of Management and Control for Complex Systems, Institute of Automation, Chinese Academy of Sciences, Beijing, People's Republic of China.
authors.forename: Xin
authors.initials: X
authors.lastname: Yang
authors.affiliation: Department of Biomedical Engineering, College of Engineering, Peking University, Beijing People's Republic of China.
authors.forename: Zhifei
authors.initials: Z
authors.lastname: Dai
authors.affiliation: Key laboratory of Molecular Imaging, The state Key Laboratory of Management and Control for Complex Systems, Institute of Automation, Chinese Academy of Sciences, Beijing, People's Republic of China.
authors.forename: Jie
authors.initials: J
authors.lastname: Tian
mesh_terms: D020533:Angiogenesis Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001557:Benzenesulfonates / Q000737:chemistry; D045744:Cell Line, Tumor / Q000187:drug effects; D015179:Colorectal Neoplasms / Q000098:blood supply / Q000188:drug therapy*; D043169:Endostatins / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D005453:Fluorescence; D006801:Humans; D007211:Indoles / Q000737:chemistry; D019344:Lactic Acid / Q000737:chemistry; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D057054:Molecular Imaging / Q000379:methods; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D010455:Peptides / Q000737:chemistry; D011091:Polyesters; D011108:Polymers / Q000737:chemistry; D011994:Recombinant Proteins; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: D020533:Angiogenesis Inhibitors; D001557:Benzenesulfonates; D043169:Endostatins; C562366:IRDye 800CW; D007211:Indoles; D010455:Peptides; D011091:Polyesters; D011108:Polymers; D011994:Recombinant Proteins; D019344:Lactic Acid; C033616:poly(lactide); C522911:endostar protein
keywords: Endostar; GX1 peptide; IRDye 800CW; angiogenesis; colorectal cancer; molecular imaging