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Preparation method and purpose of Exendin-4 coupling superparamagnetic iron oxide nano particle

An iron oxide nano- and superparamagnetic technology, applied in iron oxide, iron oxide/iron hydroxide, nanotechnology, etc., can solve the problems of short half-life, low spatial resolution of radionuclide imaging, and fast metabolism of contrast agents.

Inactive Publication Date: 2011-11-23
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The nuclides used in previous international literature reports (such as 111 In) label exendin-4 to achieve targeted imaging of insulinoma, but radionuclide imaging has defects such as low spatial resolution, fast metabolism and short half-life of contrast agent in vivo

Method used

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  • Preparation method and purpose of Exendin-4 coupling superparamagnetic iron oxide nano particle
  • Preparation method and purpose of Exendin-4 coupling superparamagnetic iron oxide nano particle
  • Preparation method and purpose of Exendin-4 coupling superparamagnetic iron oxide nano particle

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Embodiment 1

[0053]Embodiment 1, a kind of preparation method of the superparamagnetic iron oxide nanoparticle (SPIO-exendin4 nanoparticle) of exendin-4 coupling, carries out following steps successively:

[0054] 1), under the protection of inert gas Ar, at room temperature FeCl 3 ·6H 2 O and FeCl 2 4H 2 O was dissolved in polyethylene glycol 600 (PEG600) at a molar ratio of 2:1 to obtain a tan solution; FeCl 3 ·6H 2 The molar concentration of O in the tan solution was 0.05M.

[0055] 2) Under the protection of inert gas Ar, the yellow-brown solution obtained in the above step 1) was heated to 125° C., a certain amount of deionized water and EDEA were added, and the temperature was kept at 125° C. for 30 minutes to obtain a black suspension. where deionized water and FeCl 3 ·6H 2 The molar ratio of O is 20:1, EDEA and FeCl 3 ·6H 2 The molar ratio of O is 300:1.

[0056] 3), cool the black suspension obtained in the above step 2) to room temperature, add toluene and centrifuge at...

Embodiment 2

[0064] Embodiment 2, a kind of preparation method of the superparamagnetic iron oxide nanoparticle (SPIO-exendin4 nanoparticle) of exendin-4 coupling, carries out following steps successively:

[0065] 1), under the protection of inert gas, at room temperature FeCl 3 ·6H 2 O and FeCl 2 4H 2 O was dissolved in polyethylene glycol 600 (PEG600) to give a tan solution; FeCl 3 ·6H 2 O and FeCl 2 4H 2 The molar ratio of O is 2:1, FeCl 3 ·6H 2 The concentration of O in the yellow-brown solution is 0.05M.

[0066] 2) Under the protection of an inert gas, heat the yellow-brown solution obtained in step 1) to 125°C, add a certain amount of deionized water and EDEA, and keep the temperature at 125°C for 30 minutes to obtain a black suspension. where deionized water and FeCl 3 ·6H 2 The molar ratio of O is 20:1, EDEA and FeCl 3 ·6H 2 The molar ratio of O was 300:1.

[0067] 3) Cool the black suspension obtained in step 2) to room temperature, add toluene and centrifuge at 50...

Embodiment 3

[0073] Embodiment 3, a kind of preparation method of the superparamagnetic iron oxide nanoparticle (SPIO-exendin4 nanoparticle) of exendin-4 coupling, carries out following steps successively:

[0074] 1), under the protection of inert gas, at room temperature FeCl 3 ·6H 2 O and FeCl 2 4H 2 O was dissolved in polyethylene glycol 600 (PEG600) to give a tan solution; FeCl 3 ·6H 2 O and FeCl 2 4H 2 The molar ratio of O is 2:1, FeCl 3 ·6H 2 The concentration of O in the yellow-brown solution is 0.1M.

[0075] 2) Under the protection of an inert gas, heat the above yellow-brown solution to 135°C, add a certain amount of deionized water and EDEA, and keep it at 135°C for 40 minutes to obtain a black suspension; deionized water and FeCl 3 ·6H 2 The molar ratio of O is 15:1, EDEA and FeCl 3 ·6H 2 The molar ratio of O is 200:1.

[0076] 3) Cool the black suspension obtained from the reaction to room temperature, add toluene and centrifuge at 5000 rpm, remove the supernatan...

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Abstract

The invention discloses a preparation method of an Exendin-4 coupling superparamagnetism iron oxide nanometer particle. A high temperature hydrolysis of metal alkoxide chelate is employed to prepare an SPIO (superparamagnetic iron oxide) nano particle; an APS ((3-aminopropyl) trimethoxysilane) is employed to carry out silanization modification on the SPIO, and PEG (polyethylene glycol) is employed to carry out a surface coating on an APS-SPIO particle to obtain a PEG-SPIO; an NHS / EDC (N-Hydroxysuccinimide / N-ethyl-N-(3-(dimethylamino)propyl)carbodiimide) method is further employed to couple the Exendin-4 on the PEG-SPIO, so as to obtain a nano-material SPIO-exendin-4 with beta cell targeting. The SPIO-exendin-4 prepared by the method of the invention can be applied to targeting imaging of insulinome and can increase mark efficiency of the SPIO to a beta cell.

Description

technical field [0001] The invention belongs to the technical field of biology and medicine, and relates to material chemistry, specifically by synthesizing superparamagnetic iron oxide nanoparticles (Polyethylene glycol Coated Superparamagnetic Iron Oxide PEG-SPIO) modified by polyethylene glycol, and coupling exendin-4 to it Above, SPIO-exendin4, a superparamagnetic iron oxide nanoparticle with beta cell targeting, was prepared, and this contrast agent was used to target insulinomas with high expression of glucagon-like peptide-1 (GLP-1) receptor imaging. The invention also relates to the application of the material to beta cells in vitro. Background technique [0002] Insulinoma is an endocrine tumor derived from beta cells. Although its incidence rate is low (1-4 / 106), it is the most common pancreatic endocrine tumor. Insulinomas are mostly sporadic, solid and benign small tumors (mostly less than 2.0 cm in diameter) confined to the pancreas. Surgery is the standard t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C01G49/06G01N24/08B82Y30/00B82Y40/00
Inventor 吴育连张波翟传鑫
Owner ZHEJIANG UNIV
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