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Preparation and application of a rgd@bbn dual-targeting MR/optical bimodal molecular probe

A molecular probe and bimodal technology, applied in the field of preparation of RGD@BBN dual-targeting MR/optical dual-modal molecular probe, can solve the problem of inconsistency and inhomogeneity of receptor type or expression level, tumor cell surface Receptor heterogeneity and other issues, to achieve excellent biocompatibility and biodegradability, excellent performance, and large tissue penetration depth

Inactive Publication Date: 2017-12-19
GUANGZHOU FIRST PEOPLES HOSPITAL (GUANGZHOU DIGESTIVE DISEASE CENT GUANGZHOU FIRST PEOPLES HOSPITAL GUANGZHOU MEDICAL UNIV THE SECOND AFFILIATED HOSPITAL OF SOUTH CHINA UNIV OF TECH)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the process of tumor growth, the receptors on the surface of tumor cells will show heterogeneity and inhomogeneity, even in patients with the same tumor, the types or expression levels of receptors expressed in tumor tissues will be inconsistent

Method used

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  • Preparation and application of a rgd@bbn dual-targeting MR/optical bimodal molecular probe
  • Preparation and application of a rgd@bbn dual-targeting MR/optical bimodal molecular probe
  • Preparation and application of a rgd@bbn dual-targeting MR/optical bimodal molecular probe

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Effect test

Embodiment 1

[0051] A method for preparing RGD@BBN dual-targeted MR / optical dual-mode molecular probes, comprising the following steps:

[0052] (1) Preparation of superparamagnetic iron oxide nanoparticles (SPIO) solution:

[0053] Weigh 3100mg FeCl·6H 2 O with 2100mg FeSO 4 ·7H 2 O, dissolved in 40mL of deionized water, fully stirred to mix and dissolve; transfer the above solution to a three-neck round bottom flask, put in a magnetic stirrer, and place it on a constant temperature heating magnetic stirrer; pass in nitrogen, heat in a water bath at 25°C, and Add 0.15mmol / L HCl solution to adjust the pH to about 2. After mixing evenly, add 20mL of 20% concentrated ammonia water. After 30min, raise the temperature to 70°C and continue the reaction for 1h to obtain a dark brown turbid solution. Wash it with deionized water for 6 to pH 7 or so; then dissolved in 800mL deionized water, and placed in an ultrasonic cleaner for 1 hour to obtain a superparamagnetic iron oxide nanoparticle SPIO...

Embodiment 2

[0062] A method for preparing RGD@BBN dual-targeted MR / optical dual-mode molecular probes, comprising the following steps:

[0063] (1) Preparation of superparamagnetic iron oxide nanoparticles (SPIO) solution:

[0064] Weigh 4090mg of FeCl 6H 2 O with 2100mg of FeSO 4 ·7H 2 O, dissolved in 40mL of deionized water, fully stirred to mix and dissolve; transfer the above solution to a three-neck round-bottomed flask, put a magnetic stirrer, and place it on a constant temperature heating magnetic stirrer; Add 0.35mmol / L HCl solution to adjust the pH to about 3. After mixing evenly, add 30mL of 25% concentrated ammonia water. After 30min, raise the temperature to 85°C and continue the reaction for 1h to obtain a dark brown turbid liquid; wash with deionized water for 7 The pH is about 8; then dissolved in 800mL deionized water, and placed in an ultrasonic cleaner for 1 hour to obtain a superparamagnetic iron oxide nanoparticle SPIO solution with a concentration of 1.5mg / mL;

[...

Embodiment 3

[0072] A method for preparing RGD@BBN dual-targeted MR / optical dual-mode molecular probes, comprising the following steps:

[0073] (1) Preparation of superparamagnetic iron oxide nanoparticles (SPIO) solution:

[0074] Weigh 6140mg of FeCl·6H 2 O with 2100mg of FeSO 4 ·7H 2 O, dissolved in 40mL of deionized water, fully stirred to mix and dissolve; transfer the above solution to a three-necked round-bottomed flask, put a magnetic stirrer, and place it on a constant temperature heating magnetic stirrer; Add 0.5mmol / L HCl solution to adjust the pH to about 4. After mixing evenly, add 40mL of 30% concentrated ammonia water. After 30min, heat up to 90°C and continue the reaction for 1h to obtain a dark brown turbid liquid; under the adsorption of an external magnetic field , washed 10 times with deionized water until the pH is about 8; then dissolved in 800mL deionized water, and placed in an ultrasonic cleaner for 1 hour to obtain a superparamagnetic iron oxide nanoparticle S...

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Abstract

The invention discloses the preparation and application of a RGD@BBN dual-targeting MR / optical dual-mode molecular probe. In the present invention, liposomes are used as carriers, water-soluble SPIO particles are wrapped in liposome hydrophilic core, oil-soluble QDs particles are wrapped in liposome hydrophobic phospholipid bilayer, and double-targeted RGD@ BBN ligand, preparation of RGD@BBN dual-targeting MR / optical dual-modal molecular probe. The RGD@BBN contained in the bimodal molecular probe of the present invention is inserted and fixed on the surface of the phospholipid bilayer by a self-assembly method, the preparation conditions are mild, and it is efficient and practical. The present invention wraps two different image contrast agents in a relatively independent space without changing their properties, and the prepared dual-target dual-mode molecular probe has both RGD and BBN targeting functions, and is effective for RGD or ( and) BBN receptor-positive tumors all have targeting function.

Description

technical field [0001] The invention belongs to the field of molecular imaging, and specifically relates to a preparation method and application of an RGD@BBN dual-targeting MR / optical dual-mode molecular probe. Background technique [0002] Multimodal molecular imaging technology combines different morphological and functional imaging methods, MR / optical imaging, SPECT-CT / MR imaging, optical / CT imaging, optical / PET imaging, PET / CT imaging, CT / SPECT imaging and MRI / PET imaging is a common combination of multimodal imaging techniques, of which MR / optical imaging is the most widely used. [0003] In the construction of molecular probes, the commonly used tumor molecular imaging probes targeting a single target must have cell surface targets (receptors) that are specifically highly expressed in tumor tissues but not or lowly expressed in normal tissues. However, during the growth of tumors, the receptors on the surface of tumor cells will be heterogeneous and inhomogeneous. E...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/18A61K49/00
Inventor 杨蕊梦江新青唐文洁韦敏燕杨惠康
Owner GUANGZHOU FIRST PEOPLES HOSPITAL (GUANGZHOU DIGESTIVE DISEASE CENT GUANGZHOU FIRST PEOPLES HOSPITAL GUANGZHOU MEDICAL UNIV THE SECOND AFFILIATED HOSPITAL OF SOUTH CHINA UNIV OF TECH)
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