title: Carrier-free, functionalized pure drug nanorods as a novel cancer-targeted drug delivery platform.
abstract: A one-dimensional drug delivery system (1D DDS) is highly attractive since it has distinct advantages such as enhanced drug efficiency and better pharmacokinetics. However, drugs in 1D DDSs are all encapsulated in inert carriers, and problems such as low drug loading content and possible undesirable side effects caused by the carriers remain a serious challenge. In this paper, a novel, carrier-free, pure drug nanorod-based, tumor-targeted 1D DDS has been developed. Drugs are first prepared as nanorods and then surface functionalized to achieve excellent water dispersity and stability. The resulting drug nanorods show enhanced internalization rates mainly through energy-dependent endocytosis, with the shape-mediated nanorod (NR) diffusion process as a secondary pathway. The multiple endocytotic mechanisms lead to significantly improved drug efficiency of functionalized NRs with nearly ten times higher cytotoxicity than those of free molecules and unfunctionalized NRs. A targeted drug delivery system can be readily achieved through surface functionalization with targeting group linked amphipathic surfactant, which exhibits significantly enhanced drug efficacy and discriminates between cell lines with high selectivity. These results clearly show that this tumor-targeting DDS demonstrates high potential toward specific cancer cell lines.
authors.affiliation: Nano-organic Photoelectronic Laboratory and Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, People's Republic of China.
authors.forename: Yanan
authors.initials: Y
authors.lastname: Li
authors.forename: Yinlong
authors.initials: Y
authors.lastname: Yang
authors.forename: Feifei
authors.initials: F
authors.lastname: An
authors.forename: Zhuang
authors.initials: Z
authors.lastname: Liu
authors.forename: Xiujuan
authors.initials: X
authors.lastname: Zhang
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Zhang
mesh_terms: D001672:Biocompatible Materials / Q000494:pharmacology; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D004705:Endocytosis / Q000187:drug effects; D006801:Humans; D008422:Materials Testing; D018613:Microscopy, Confocal; D043942:Nanotubes / Q000737:chemistry* / Q000633:toxicity / Q000648:ultrastructure; D009369:Neoplasms / Q000188:drug therapy*; D017239:Paclitaxel / Q000494:pharmacology / Q000627:therapeutic use; D011208:Powders; D011956:Receptors, Cell Surface / Q000378:metabolism; D013696:Temperature; D013997:Time Factors; D014867:Water / Q000737:chemistry
chemical_list: D001672:Biocompatible Materials; D004337:Drug Carriers; D011208:Powders; D011956:Receptors, Cell Surface; D014867:Water; D017239:Paclitaxel