Preparation method and application of RGD@BBN double-targeted MR (magnetic resonance)/optical dual-mode molecular probe

A molecular probe and bimodal technology, applied in the field of preparation of RGDBBN dual-targeting MR/optical dual-modal molecular probe, can solve inhomogeneity, inconsistent receptor types or expression levels, and receptors on the surface of tumor cells Heterogeneity and other issues, to achieve the effect of excellent performance, excellent biocompatibility and biodegradability, and large tissue penetration depth

Inactive Publication Date: 2015-11-25
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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  • Abstract
  • Description
  • Claims
  • Application Information

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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 method and application of RGD@BBN double-targeted MR (magnetic resonance)/optical dual-mode molecular probe
  • Preparation method and application of RGD@BBN double-targeted MR (magnetic resonance)/optical dual-mode molecular probe
  • Preparation method and application of RGD@BBN double-targeted MR (magnetic resonance)/optical dual-mode molecular probe

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Embodiment 1

[0051] A method for preparing an RGDBBN dual-targeted MR / optical dual-mode molecular probe, comprising the steps of:

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

[0053] Weigh 3100mgFeCl·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 liquid, which is washed 6 times with deionized water. until the pH is about 7; then dissolved in 800mL deionized water, and placed in an ultrasonic cleaner for 1 hour to obtain a superparamagnetic iron oxide nanop...

Embodiment 2

[0062] A method for preparing an RGDBBN dual-targeted MR / optical dual-mode molecular probe, comprising the steps of:

[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 it with deionized water for 7 times 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 SPIO solution with a concentration of 1.5mg...

Embodiment 3

[0072] A method for preparing an RGDBBN dual-targeted MR / optical dual-mode molecular probe, comprising the steps of:

[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, raise the temperature to 90°C and continue the reaction for 1h to obtain a dark brown turbid liquid; under the adsorption of an external magnetic field, Wash with deionized water 10 times until the pH is about 8; then dissolve in 800mL deionized water, and place in an ultrasonic cleaner for 1 hour to obtain a superparamagnetic iron oxide nanoparticl...

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Abstract

The invention discloses a preparation method and application of an RGD@BBN double-targeted MR (magnetic resonance)/optical dual-mode molecular probe, wherein the RGD@BBN double-targeted MR/optical dual-mode molecular probe is prepared by the following steps: coating water-soluble superparamagnetic iron oxide ( SPIO) particles in hydrophilic core of lipidosome and coating oil-soluble QDs particles in hydrophobic lipid bilayer of the lipidosome by taking lipidosome as a carrier, and linking a double-targeted RGD@BBN ligand by virtue of a post-interpolation method. The RGD@BBN contained in the dual-mode molecular probe disclosed by the invention is interpolated and immobilized on the surface of the lipid bilayer by virtue of self-assembly, and the preparation method is mild in condition and is efficient and practical. According to the invention, a relatively independent space is coated by two different image contrast agents without changing the properties of the image contrast agents; and the prepared double-target dual-mode molecular probe, which simultaneously has RGD and BBN targeting functions, has targeting functions on RGD or (and) BBN receptor-positive tumors.

Description

technical field [0001] The invention belongs to the field of molecular imaging, and in particular relates to a preparation method and application of an RGDBBN 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 Applications(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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