US 12,642,766 B2 · EDB-FN as biomarker of cancer and/or brain disease and nanodrug delivery system targeting same

Abstract

The present invention relates to a drug delivery system with a micelle structure comprising a PEG2000-DSPE polymerized lipid and an APTEDB-PEG2000-DSPE polymer, and a preparation method thereof. The drug delivery system targets extra-domain B of fibronectin (EDB-FN), which is overexpressed in a brain tumor, and can pass through the blood-brain barrier (BBB) or the blood-brain tumor barrier (BBTB) to deliver a drug specifically to the brain tumor cells. In addition, the present invention can provide a pharmaceutical composition for diagnosing or treating a brain tumor, comprising the drug-loaded drug delivery system as an active ingredient. The composition can be accumulated inside the brain tumor and incorporated into the tumor cells to specifically inhibit tumor growth, and thus can be efficiently utilized for diagnosing or treating a brain tumor.

Claims8

Dependent claims

A method of producing a brain tumor-specific drug delivery system, the method comprising steps of:

(1) mixing APTEDB containing cysteine residues and Mal-PEG2000-DSPE in an organic solvent in a molar ratio of 1:2 and inducing polymerization;
(2) obtaining an APTEDB-PEG2000-DSPE polymer from the mixed solution of step (1);
(3) mixing the APTEDB-PEG2000-DSPE polymer and PEG2000-DSPE polymerized lipid in one or more solvents selected from the group consisting of water, PBS, HBS, and HBG to induce formation of a micelle structure;
and
(4) filtering the mixed solution of step (3) and purifying the micellar structure to yield micelles having a hydrodynamic diameter of 7-12 nm and a zeta potential of −8.2 to −12.8 mV as measured by dynamic light scattering, wherein the APTEDB of step (1) is an aptide that exhibits specific binding ability to extradomain B of fibronectin (EDB-FN) gene (Entrez Gene ID:
2335).

3 more elements

Dependencies are inferred from the claim text.

Facts

Application

17/800,202Filed 17 Feb 2021

Priority

KR 10-2020-002053719 Feb 2020

Published

US 2023/0109491 A16 Apr 2023

Granted

2 Jun 2026

Term ends

Not estimatedThe source records don’t support an estimate.

Classification10 codes

A61K 9/1075
Emulsions ; Emulsion preconcentrates; Micelles: microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of…
A61K 47/62
The non-active ingredient being a modifying agent: the modifying agent being a protein, peptide or polyamino acid
A61K 47/6909
The form being a microemulsion, nanoemulsion or micelle: micelles formed by phospholipids
A61K 49/08
Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations: characterised by the carrier

EDB-FN as biomarker of cancer and/or brain disease and nanodrug delivery system targeting same

Life of this patent

EDB-FN as biomarker of cancer and/or brain disease and nanodrug delivery system targeting same

Life of this patent

Abstract

Claims8