title: Delivery of paclitaxel using PEGylated graphene oxide as a nanocarrier.
abstract: Paclitaxel (PTX) is an extensively used potent chemotherapy drug; however, low water solubility, poor bioavailability, and emergence of drug resistance in patients limited its biological application. In this report, we proposed a new drug delivery system for cancer therapy based on graphene oxide (GO), a novel 2D nanomaterial obtained from the oxidation of natural graphite, to improve the utilization rate of PTX. PTX was first connected to biocompatible 6-armed poly(ethylene glycol), followed by covalent introduction into the surface of GO sheets via a facile amidation process under mild conditions, affording the drug delivery system, GO-PEG-PTX (size 50-200 nm). GO-PEG nanosized carrier could quickly enter into human lung cancer A549 and human breast cancer MCF-7 cells verified by inverted fluorescence microscope using fluorescein isothiocyanate as probe. This nanocarrier was nontoxic to A549 and MCF-7 cells without linking with PTX. Nevertheless, GO-PEG-PTX showed remarkably high cytotoxicity to A549 and MCF-7 cells in a broad range of concentration of PTX and time compared to free PTX. This kind of nanoscale drug delivery system based on PEGylated GO may find widespread application in biomedicine.
authors.affiliation: Key Laboratory of Synthetic and Self-Assembly Chemistry for Organic Functional Molecules, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 345 Lingling Road, Shanghai 200032, People's Republic of China.
authors.forename: Zhiyuan
authors.initials: Z
authors.lastname: Xu
authors.forename: Shaojia
authors.initials: S
authors.lastname: Zhu
authors.forename: Mingwei
authors.initials: M
authors.lastname: Wang
authors.forename: Yongjun
authors.initials: Y
authors.lastname: Li
authors.forename: Ping
authors.initials: P
authors.lastname: Shi
authors.forename: Xiaoyu
authors.initials: X
authors.lastname: Huang
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000295:instrumentation* / Q000379:methods; D006108:Graphite / Q000737:chemistry*; D006801:Humans; D061986:MCF-7 Cells; D010087:Oxides / Q000737:chemistry*; D017239:Paclitaxel / Q000737:chemistry / Q000494:pharmacology*; D010316:Particle Size
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D010087:Oxides; D006108:Graphite; D017239:Paclitaxel
keywords: PEG; drug delivery; graphene oxide; paclitaxel