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US 11,179,474 B1Granted
Nanoparticle-based liver-targeting therapy and imaging
AssigneeMidatech Limited
InventorsAfrica Garcia Barrientos, Esther de Torres Dominguez
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Abstract
The invention provides a nanoparticle comprising: a core comprising a metal and/or a semiconductor; and a plurality of ligands covalently linked to the core, wherein said ligands comprise: at least one liver-targeting ligand; at least one payload ligand comprising a bioactive agent; and at least one dilution ligand comprising a carbohydrate. Also provided are pharmaceutical compositions comprising the nanoparticles, medical uses thereof, including in the treatment and imaging of liver cancers, and processes for the production of the nanoparticles.
Claims16
A nanoparticle comprising:
- a core comprising a metal, wherein the diameter of the core is in the range 1 nm to 5 nm, as determined by transmission electron microscopy (TEM);
- and
- a plurality of ligands covalently linked to the core, wherein said ligands comprise:
- (i) at least one liver-targeting ligand which is an asialoglycoprotein receptor (ASGPR) binding agent comprising a carbohydrate, wherein the liver-targeting ligand is covalently linked to the core via a liver-targeting ligand linker that comprises:
- —(CH2)n—, wherein n is at least 5;
- and/or
- —(OCH2CH2)m—, wherein m is at least 3;
- (ii) at least one payload ligand comprising a bioactive agent which is a small molecule organic compound that is cytotoxic;
- and
- (iii) a plurality of dilution ligands each comprising a carbohydrate which is a monosaccharide, wherein said dilution ligands are each covalently bound to the core via a dilution ligand linker having a chain length of 2 to 4 atoms, and
- wherein the total number of said plurality of ligands covalently linked to the core is at least 20, and wherein the diameter of the nanoparticle including its ligands is not more than 50 nm, and wherein said dilution ligands make up between 10% and 70% of the total number of ligands of the nanoparticle.
8 more elements
Dependencies are inferred from the claim text.