title: Dual-acting, function-responsive, and high drug payload nanospheres for combining simplicity and efficacy in both self-targeted multi-drug co-delivery and synergistic anticancer effect.
abstract: Recently, the global trend in the field of nanomedicine has been toward the design of highly sophisticated drug delivery systems with specific targeting and synergistic therapeutic functions for improving therapeutic efficacy. But offering sophistication generally increases their complexity that might be disadvantageous in pharmaceutical development. We hypothesize that using a macromolecular prodrug with a dual role will be conductive to integrating its dual function into self-targeted multidrug co-delivery and combination cancer therapy. In this paper, the on-off switching function-responsive, macromolecular methotrexate (MTX) prodrug-self-targeted, controlled-/sustained-release, and high drug-loading hydroxylcamptothecin (HCPT) drug nanospheres were prepared and characterized. The self-targeting system can co-deliver multi-drug to different action sites with distinct anticancer mechanisms to specifically target folate receptors-overexpressing cancer cells with synergistic therapeutic efficiency.
authors: Department of Biomaterials, College of Materials, Xiamen University, Xiamen 361005, China.
authors: Yang
authors: Y
authors: Li
authors: Department of Biomaterials, College of Materials, Xiamen University, Xiamen 361005, China; The State Key Laboratory of Physical Chemistry of Solid Surface, Department of Chemistry, College of Chemistry & Chemical Engineering, Xiamen University, Xiamen 361005, China.
authors: Jinyan
authors: J
authors: Lin
authors: Department of Pharmacy, School of Pharmaceutical Science, Xiamen University, Xiamen 361005, China.
authors: Guihua
authors: G
authors: Liu
authors: Department of Pharmacy, School of Pharmaceutical Science, Xiamen University, Xiamen 361005, China.
authors: Jinyuan
authors: J
authors: Ma
authors: The First affiliated Hospital of Xiamen University, Xiamen 361003, China.
authors: Liya
authors: L
authors: Xie
authors: Department of Physical, Changji University, Changji 831100, China.
authors: Fuqiang
authors: F
authors: Guo
authors: Department of Pharmacy, School of Pharmaceutical Science, Xiamen University, Xiamen 361005, China. Electronic address: zhuxuan@xmu.edu.cn.
authors: Xuan
authors: X
authors: Zhu
authors: Department of Biomaterials, College of Materials, Xiamen University, Xiamen 361005, China; Department of Physical, Changji University, Changji 831100, China. Electronic address: houzhenqing@xmu.edu.cn.
authors: Zhenqing
authors: Z
authors: Hou
mesh_terms: D000818:Animals; D002166:Camptothecin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D065546:Drug Liberation; D004355:Drug Stability; D020128:Inhibitory Concentration 50; D008727:Methotrexate / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D051379:Mice; D054118:Nanospheres / Q000008:administration & dosage* / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry; D011355:Prodrugs / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays
chemical_list: D004337:Drug Carriers; D011355:Prodrugs; D011092:Polyethylene Glycols; D002166:Camptothecin; D008727:Methotrexate
keywords: Drug nanoparticles; Dual acting; Multi-drug co-delivery; Synergistic anticancer effect