Multifunctional tumor imaging agent, preparation method and application

A tumor imaging agent, multifunctional technology, applied in the field of tumor imaging agents

Inactive Publication Date: 2012-08-01
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, most of the drugs widely used in clinical tumor diagnosis and treatment are non-selective drugs, which are widely distributed in the body, and conventional therapeutic doses can produce significant toxic and side effects on normal tissues and organs, resulting in patients' intolerance, so the tumor resistance of drugs is increased. Selectivity, reducing its aggregation at non-targeted sites is the key to improving the efficacy of anticancer drugs

Method used

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  • Multifunctional tumor imaging agent, preparation method and application
  • Multifunctional tumor imaging agent, preparation method and application
  • Multifunctional tumor imaging agent, preparation method and application

Examples

Experimental program
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Embodiment 1

[0029] Embodiment 1 (example of the most expensive preparation conditions) : Magnetic nano-Fe with a particle size of 20 nm 3 o 4 (40 mg) and tetramethoxysilane (TEOS ) (80mg) were mixed at a mass ratio of 1:2 and ultrasonically dispersed in 80 mg chloroform (Fe 3 o 4 The mass ratio of chloroform to chloroform is 1:2), then add 0.5M cetyltrimethylammonium bromide (CTAB) aqueous solution 0.8ml, then add water 2ml and 2 M NaOH solution 0.4g (where NaOH and TEOS The mass ratio is 1:5), and the temperature is controlled at the optimal 70 oC to obtain solution A; another part of TEOS (120mg) and rhodamine B isothiocyanate (RBITC) (60mg) are mixed at a mass ratio of 2:1 to prepare Solution B; solution B is added in solution A, then add the 20% ethyl acetate of reaction solution volume, add APS (200mg) (APS: Fe 3 o 4 The mass ratio is 5:1), stirred for 3 h, magnetically separated, and the solid was washed twice with ethanol and water respectively to obtain the encapsulated flu...

Embodiment 2

[0033] Example 2: Magnetic nano-Fe with a particle size of 20 nm 3 o 4 (40 mg) and TEOS (40mg) were mixed at a mass ratio of 1:1 and ultrasonically dispersed in 40 mg chloroform (Fe 3 o 4 The mass ratio of chloroform to chloroform is 1:1), then add 0.12ml of 0.5M cetyltrimethylammonium bromide (CTAB) aqueous solution, then add 0.3ml of water and 0.1g of 2M NaOH solution (wherein NaOH and TEOS The mass ratio of 1:1), the temperature was controlled at the optimal 70 oC to prepare solution A; another part of TEOS (20mg) and RBITC (20mg) was mixed at a mass ratio of 1:1 to make solution B; solution B was added In solution A, add 5% ethyl acetate of reaction liquid volume again, add APS (400mg) (APS: Fe 3 o 4 The mass ratio was 10:1), stirred for 3 h, magnetically separated, and the solid was washed twice with ethanol and water respectively to obtain the encapsulated fluorescent dye rhodamine B isothiocyanate (RBITC) and porous magnetic nanometer ferric oxide as the core, di...

Embodiment 3

[0036] Example 3: Magnetic nano-Fe with a particle size of 20 nm 3 o 4 (60 mg) and TEOS (240mg) were mixed at a mass ratio of 1:6 and ultrasonically dispersed in 600 mg chloroform (Fe 3 o 4 To chloroform mass ratio 1:10), add 0.5M cetyltrimethylammonium bromide (CTAB) aqueous solution 1.2 ml, then add water 240 ml and 2 M NaOH solution 2.4 g (wherein NaOH and The mass ratio of TEOS was 1:10), and the temperature was controlled at the optimal 30 oC to prepare solution A; another part of TEOS (120 mg) and RBITC (120 mg) was mixed at a mass ratio of 1:1 to make solution B; Solution B was added in solution A, then added 40% ethyl acetate of reaction solution volume, added APS (60mg) (APS: Fe 3 o 4 The mass ratio was 1:1), stirred for 3 h, magnetically separated, and the solid was washed twice with ethanol and water respectively to obtain the encapsulated fluorescent dye rhodamine B isothiocyanate (RBITC) and porous magnetic nanometer ferric oxide as the core, di Silica-she...

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Abstract

The invention discloses a multifunctional tumor imaging agent, a preparation method and application, and belongs to the field of tumor imaging agents. The tumor imaging agent has tumor target and magnetic resonance imaging and anti-tumor properties. Fe3O4 is used as a nucleus; and nano particles coated with fluorescent dye rhodamine isothiocyanate B and porous magnetic nano ferroferric oxide which serve as nuclei and silicon dioxide serving as a shell are prepared by a micro-emulsion method. Tumor targeting arginine-glycine-aspartic acid (RGD) peptide and methoxy polyethylene glycol are modified on the surface of the SiO2, and the tumor targeting multifunctional composite imaging agent is finally obtained. The imaging agent has tumor targeting peptide induced tumor cell active targeting property, can be used as a magnetic resonance imaging identification agent for tumor cells and normal cells, can be applied to clinical magnetic resonance imaging monitoring treatment medicaments, and realizes constant monitoring of a tumor treatment process, but the conventional anti-tumor medicament applied in clinic only has tumor inhibiting performance and cannot realize real-time monitoring ofthe medicament treatment process.

Description

technical field [0001] The invention relates to a multifunctional tumor imaging agent and its preparation technology, belonging to the field of tumor imaging agents, in particular to a targeted tumor imaging agent and its preparation method and application. [0002] Background technique [0003] Due to the excessive proliferation of tumor cells and the invasion and metastasis of normal tissues, cancer has become a serious disease that threatens human health. However, most of the drugs widely used in clinical tumor diagnosis and treatment are non-selective drugs, which are widely distributed in the body, and conventional therapeutic doses can produce significant toxic and side effects on normal tissues and organs, resulting in patients' intolerance, so the tumor toxicity of drugs is increased. Selectivity and reducing its aggregation in non-targeted sites are the keys to improving the efficacy of antitumor drugs. Targeted drugs can enter the target area to the maximum exten...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/12
Inventor 陈秋云陶艮平刘颖奇
Owner JIANGSU UNIV
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