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Nanoparticle-based liver-targeting therapy and imaging
专利权人:
Midatech Limited
发明人:
Africa Garcia Barrientos,Esther de Torres Domínguez
申请号:
GB201513103
公开号:
GB2541166A
申请日:
2015.07.24
申请国别(地区):
GB
年份:
2017
代理人:
摘要:
A nanoparticle comprising: a core comprising a metal and/or a semiconductor, preferably gold, and a plurality of ligands covalently linked to the core, wherein the ligands comprise (i) at least one liver-targeting ligand; (ii) at least one payload ligand comprising a bioactive agent; and (iii) at least one dilution ligand comprising a carbohydrate, is provided. Preferably the liver-targeting ligand comprises lactose which is covalently linked to the core via a first linker which preferably comprises -(OCH2CH2)m-(CH2)n- where m = 1 to 10 and n = 1 to 15 and is preferably bound to the core via a terminal sulphur atom. Preferably the payload ligand comprises a therapeutic agent selected from doxorubicin, irinotecan, platinum (II), platinum (IV), temozolomide, carmustine, camptothecin, docetaxel, and sorafenib. Preferably the at least one dilution ligand comprises a monosaccharide, in particular glucose or galactose, which is preferably covalently bound to the core via a third linker which comprises -(CH2)n- where n = 2 to 3, which is preferably bound to the core via a terminal sulphur atom. Preferably the nanoparticle comprises a plurality of ligands comprising (iv) a lactose-containing ligand; (v) a doxorubicin-containing ligand; and (vi) a monosaccharide ligand comprising galactose or glucose. Preferably the nanoparticle is for use in the treatment of a liver disorder in a mammalian subject, in particular hepatocellular carcinoma.
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