期刊
NANOMEDICINE-NANOTECHNOLOGY BIOLOGY AND MEDICINE
卷 7, 期 1, 页码 80-87出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.nano.2010.07.001
关键词
PEG; Click chemistry; Lactose; Targeting; Acid-cleavable linkage
资金
- Natural Sciences and Engineering Research Council of Canada (NSERC)
Hepatocyte-targeting and shell cross-linked nanoparticles with lactose moiety on the surface and doxorubicin (DOX) in the core were prepared from lactose-PEG-DOX conjugate. The process consists of the synthesis of a novel alpha-hydrazine-omega-propargyl poly(ethylene glycol) (PEG) with a double bond in the PEG backbone, followed by the bonding of a lactose molecule containing an azide group to the omega-end of PEG via click chemistry, and finally, the conjugation of DOX to the alpha-end of PEG via an acid-labile, hydrazone linkage. The resultant conjugate can be self-assembled into nanoparticles. Thiolated tri(ethylene glycol) was introduced into the shell of nanoparticles as a cross-linking agent. The release of DOX is more rapid from lactose-PEG-DOX at pH 5.0 than at pH 7.4. Fluorescent microscope studies suggest that the lactose-DOX nanoparticles are internalized by hepatoma cells through a lactose receptor-mediated mechanism, whereas the lactose-free nanoparticles are not endocytosed as rapidly as lactose-DOX nanoparticles. MTT assay also shows that lactose-DOX nanoparticles have a stronger inhibition against hepatoma cells than DOX nanoparticles and pure DOX. From the Clinical Editor: In this basic science study, a highly efficient targeted doxorubicin delivery method to hepatocytes is presented. (C) 2011 Elsevier Inc. All rights reserved.
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