title: Self-Targeted, Shape-Assisted, and Controlled-Release Self-Delivery Nanodrug for Synergistic Targeting/Anticancer Effect of Cytoplasm and Nucleus of Cancer Cells.
abstract: We constructed 10-hydroxycamptothecin (CPT) "nanodrugs" with functionalization of lipid-PEG-methotrexate (MTX) to prepare high-drug-loaded, and sustained/controlled-release MTX-PEG-CPT nanorods (NRs), in which MTX drug itself can serve as a specific "targeting ligand". The self-targeted nanodrug can codeliver both CPT and MTX drugs with distinct anticancer mechanisms. Furthermore, MTX-PEG-CPT NRs significantly reduced burst release, improved blood circulation and tumor accumulation, enhanced cellular uptake, and synergistically increased anticancer effect against tumor cells compared with MTX-PEG-CPT nanospheres (NSs) and either both free drugs or individual free drug. Therefore, the synergistic targeting/therapeuticy nano-multi-drug codelivery assisted by shape design may advantageously offer a promising new strategy for nanomedicine.
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Jinyan
authors.initials: J
authors.lastname: Lin
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Huang
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Yanxiu
authors.initials: Y
authors.lastname: Li
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Xiangrui
authors.initials: X
authors.lastname: Yang
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Hongjie
authors.initials: H
authors.lastname: Wu
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Shichao
authors.initials: S
authors.lastname: Wu
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Liya
authors.initials: L
authors.lastname: Xie
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Lizong
authors.initials: L
authors.lastname: Dai
authors.affiliation: Department of Biomaterials and Department of Materials Science and Engineering, College of Materials, §Fujian Provincial Key Laboratory of Fire Retardant Materials, College of Materials, ⊥Department of Chemistry, College of Chemistry & Chemical Engineering, ∥Department of Pharmacy, School of Pharmaceutical Science, and #The First Affiliated Hospital of Xiamen University, Xiamen University , Xiamen 361005, China.
authors.forename: Zhenqing
authors.initials: Z
authors.lastname: Hou
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002467:Cell Nucleus / Q000187:drug effects / Q000378:metabolism*; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations; D004357:Drug Synergism; D004705:Endocytosis / Q000187:drug effects; D005453:Fluorescence; D008727:Methotrexate / Q000494:pharmacology*; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D054118:Nanospheres / Q000737:chemistry / Q000648:ultrastructure; D043942:Nanotubes / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D017207:Rats, Sprague-Dawley
chemical_list: D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; C028098:10-hydroxycamptothecin; D002166:Camptothecin; D008727:Methotrexate
keywords: DSPE-PEG-MTX; nanodrug; self-targeted drug delivery; sustain/controlled drug release; synergistic anticancer activity