Dual-modal nano imaging drug Dex-Rho-99mTc based on glucan

A technology of -dex-rho-99mtc and rho-dex-peg-dtpa-99mtc is applied in the field of imaging medicine, imaging diagnosis, and the preparation of dual-mode nano-imaging medicine to improve biocompatibility and price The effect of low cost and easy availability of raw materials

Inactive Publication Date: 2015-04-15
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is a lack of clinical drugs that can identify and characterize the location and degree of blood-brain barrier permeability changes

Method used

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  • Dual-modal nano imaging drug Dex-Rho-99mTc based on glucan
  • Dual-modal nano imaging drug Dex-Rho-99mTc based on glucan
  • Dual-modal nano imaging drug Dex-Rho-99mTc based on glucan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] (1) Nano imaging drug carrier material Dex-NH 2 Synthesis

[0037] Dextran (200mg) with a molecular weight of 20kDa was dissolved in 7mL of 6M NaOH solution, cooled in an ice bath to 0°C, added sodium chloroacetate (503mg), reacted at 60°C for 50min, and then added dropwise to methanol to obtain a white flocculent precipitate Dex- COOH. Dex-COOH (200 mg) was dissolved in 20 ml of water (pH 3.0), and 1 ml of 2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline (EEDQ, 320 mg) in DMF was added dropwise. This solution was dropped into 0.414mL ethylenediamine, and stirred at room temperature for 4h. The reaction solution was concentrated to 3 mL by rotary evaporation, and dropped into methanol to obtain the white floc product Dex-NH 2 .Dex-NH 2 .The aqueous solution was purified by ultrafiltration three times with an ultrafiltration tube with a molecular weight cut-off of 3kDa, and the concentrated solution was freeze-dried to obtain a white flocculent solid product, which is ...

Embodiment 2

[0041] (1) Synthesis of nanoimaging drug carrier material Dex-NH 2

[0042] Dextran (200mg) with a molecular weight of 20kDa was dissolved in 7mL of 6M NaOH solution, cooled in an ice bath to 0°C, added sodium chloroacetate (503mg), reacted at 60°C for 50min, and then added dropwise to methanol to obtain a white flocculent precipitate Dex- COOH. Dex-COOH (200 mg,) was dissolved in 20 ml of water (pH 3.0), and 1 ml of 2-ethoxy-1-ethoxycarbonyl-1,2-dihydroquinoline (EEDQ, 320 mg) in DMF was added dropwise . This solution was dropped into 0.414mL ethylenediamine, and stirred at room temperature for 4h. The reaction solution was concentrated to 3 mL by rotary evaporation, and dropped into methanol to obtain the white floc product Dex-NH 2 .Dex-NH 2 .The aqueous solution was purified by ultrafiltration three times with an ultrafiltration tube with a molecular weight cut-off of 3kDa, and the concentrated solution was freeze-dried to obtain a white flocculent solid product, whic...

Embodiment 3

[0048] With the test method of Example 1, the molecular weight of the fixed carrier material Dextran is determined as 50kDa, and the molecular weight of PEG is changed to obtain the imaging drug Rho-Dex connected with 1kDa, 2kDa, 3.5kDa, 5kDa, 10kDa molecular weight PEG 50k -PEG-DTPA- 99m Tc.

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Abstract

The invention belongs to the field of molecular imaging probes and particularly relates to a preparation method of a dual-modal nano imaging drug Dex-Rho-99mTc based on glucan, and an application of the drug in imaging diagnosis. The general formula of the drug is Rho-Dex-PEG-DTPA-99mTc, wherein the Dex represents for the glucan of which the molecular weight is 10-100k, the PEG represents for polyethylene glycol of which the molecular weight is 1-10k, the Rho represents for a fluorescent group rhodamine, the DTPA is a chelating agent of an imaging nuclide and the 99mTc is a radioisotope Technetium-99 used for SPECT imaging. In the invention, the surface of the high-molecular material glucan is modified by a certain number of amino groups and the PEG, the fluorescent group and the SPECT imaging groups are connected to the glucan supporter through the amino groups and finally the drug is marked by the radioisotope [99mTc]. The drug is good in biocompatibility, is simple in the preparation method, is safe and convenient to use and can be employed in dual-modal imaging. The dual-modal nano imaging drug has wide application prospects in the biomedical fields of early diagnosis of cancer, medicine delivery under guide of imaging, noninvasive iconography curative effect evaluation and the like.

Description

technical field [0001] The invention belongs to the field of molecular imaging probes, relates to imaging drugs, in particular to a preparation method of a dual-mode nano-imaging drug based on dextran carrier and its application in imaging diagnosis. Background technique [0002] Tumor is one of the major diseases that threaten human health. An important reason for the high mortality rate of cancer at this stage is the hysteresis of tumor diagnosis. Timely and accurate diagnosis of tumors and corresponding treatment measures have important scientific and clinical significance for improving the survival rate and quality of life of cancer patients. [0003] Single photon emission computed tomography (SPECT) is a technique for imaging by detecting gamma rays emitted by radiopharmaceuticals entering specific tissues and organs in the body. This technique has the advantages of high sensitivity, rapid imaging, easy access to required nuclides, and simple labeling, and is widely ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/06A61K49/00A61K103/10
Inventor 李聪高西辉钱隽
Owner FUDAN UNIV
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