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

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

Inactive Publication Date: 2013-05-29
ZHEJIANG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Nuclides used in previous international literature reports (such as 111 In) label exendin-4 to achieve targeted imaging of insulinoma, but nuclide 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 of Exendin-4 coupling superparamagnetic iron oxide nano particle
  • Preparation method of Exendin-4 coupling superparamagnetic iron oxide nano particle
  • Preparation method of Exendin-4 coupling superparamagnetic iron oxide nano particle

Examples

Experimental program
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Embodiment 1

[0053]Embodiment 1, a preparation method of exendin-4 coupled superparamagnetic iron oxide nanoparticles (SPIO-exendin4 nanoparticles), the following steps are performed in sequence:

[0054] 1) Under the protection of inert gas Ar, 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 yellow-brown 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, heat the yellow-brown solution obtained in the above step 1) to 125°C, add a certain amount of deionized water and EDEA, and keep warm 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 5000rpm, the volume ratio of toluene to black suspen...

Embodiment 2

[0064] Embodiment 2, a preparation method of exendin-4 coupled superparamagnetic iron oxide nanoparticles (SPIO-exendin4 nanoparticles), the following steps are performed in sequence:

[0065] 1) Under the protection of inert gas, 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 warm 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.

[0067] 3) Cool the black suspension obtained in step 2) to room temperature, add toluene and centrifuge at 5000 rpm, remove the supernatant, and obta...

Embodiment 3

[0073] Embodiment 3, a preparation method of exendin-4 coupled superparamagnetic iron oxide nanoparticles (SPIO-exendin4 nanoparticles), the following steps are performed in sequence:

[0074] 1) Under the protection of inert gas, 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 supernatant, and obtain brown iron oxi...

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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 polyethylene glycol coated superparamagnetic iron oxide nanoparticles (Polyethylene glycol Coated Superparamagnetic Iron Oxide PEG-SPIO) 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 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 treatment fo...

Claims

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Application Information

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Patent Type & Authority Patents(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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