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Functionalized polyethyleneimine-wrapped nano-gold particle composite material and preparation method thereof

A technology of polyethyleneimine and nano-gold particles, which is applied in the direction of radioactive carriers, can solve the problems of large injection, low concentration of nano-contrast agents, and limited imaging effects, etc., and achieves easy operation, good pH response, charge reversal performance, The effect of the simple preparation process

Active Publication Date: 2021-09-28
NANJING TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

With the development of nanotechnology, many SPECT / CT dual-modality imaging contrast agents based on nanoparticles have been developed, which can perform imaging at the microscopic level. The concentration is still low, which limits the imaging effect. In order to achieve a more accurate imaging effect, a large amount of material needs to be injected

Method used

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  • Functionalized polyethyleneimine-wrapped nano-gold particle composite material and preparation method thereof
  • Functionalized polyethyleneimine-wrapped nano-gold particle composite material and preparation method thereof
  • Functionalized polyethyleneimine-wrapped nano-gold particle composite material and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] (1) Dissolve trityl mercaptan (5.0 g, 18.1 mmol) with ethanol-benzene mixed solvent (50 mL) with a volume ratio of 1:1, and add 9.5 mL of NaOH solution (0.9 g, 22.6 mmol), and then add 11-Bromoundecanol (4.5 g, 18 mmol) was dissolved in ethanol-benzene mixed solution (50 mL) at a volume ratio of 1:1. The mixed solution was stirred for 12 h, after which the reaction mixture was added to saturated NaHCO 3 Extracted in the solution, washed twice, separated the organic phase and transferred it to a saturated NaCl solution for extraction, washed twice, and the separated organic phase was washed with NaCl 2 SO 4 The solution obtained after drying was concentrated by a rotary evaporator to obtain a crude product, which was purified by silica gel column chromatography, using hexane-ethyl acetate at a volume ratio of 4:1 as the eluent, and the collected product was concentrated by a rotary evaporator again 1,1,1-Triphenyl-2-thia-13-carbon tridecanol is obtained.

[0081] (2) ...

Embodiment 2

[0094] (1) Dissolve trityl mercaptan (18.1mmol) in an ethanol-benzene mixed solvent with a volume ratio of 1:1, and add NaOH solution (22.6mmol), then add the ethanol-benzene solution dissolved in a volume ratio of 1:1 11-bromoundecanol (18 mmol) in the mixed solution. The mixed solution was stirred for 8 h, after which the reaction mixture was added to saturated NaHCO 3 Extracted in the solution, washed twice, separated the organic phase and transferred it to a saturated NaCl solution for extraction, washed twice, and the separated organic phase was washed with NaCl 2 SO 4 The solution obtained after drying was concentrated by a rotary evaporator to obtain a crude product, which was purified by silica gel column chromatography, using hexane-ethyl acetate at a volume ratio of 4:1 as the eluent, and the collected product was concentrated by a rotary evaporator again 1,1,1-Triphenyl-2-thia-13-carbon tridecanol is obtained.

[0095] (2) Dissolve 1,1,1-triphenyl-2-thia-13-carbo...

Embodiment 3

[0108] The difference between Example 3 and Example 2 is that the chelating agent used is 2,2',2"-(10-(2-(2,5-dioxopyrrolidine-1-oxyl)- 2-Oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-tri)triacetic acid.

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Abstract

The invention relates to a functionalized polyethyleneimine-wrapped nano-gold particle composite material and a preparation method thereof. The preparation method comprises adding EDC and hyperbranched polyethyleneimine solution to mPEG-COOH, and reacting to obtain PEI.NH 2 ‑(mPEG), then add MAL‑PEG‑SVA solution, react to get PEI.NH 2 ‑(PEG‑MAL)‑(mPEG), followed by chelating agent DTA, fluorescent marker FI, followed by chloroauric acid, NaBH 4 , get {(Au 0 ) 200 ‑PEI.NH 2 ‑FI‑DTA‑(PEG‑MAL)‑(mPEG)}PENPs, followed by addition of APAS, followed by acetylation to give {(Au 0 ) 200 ‑PEI.NHAc‑FI‑DTA‑(PEG‑APAS)‑(mPEG)}PENPs, and finally the radionuclide 99m Tc labeled on the chelating agent DTA, that is. The functionalized polyethyleneimine-coated gold nanoparticles prepared by the invention can increase the uptake of the nano-gold particles by cancer cells, and as a good SPECT / CT imaging nano-contrast agent, has potential application value in multi-modal imaging of tumors.

Description

technical field [0001] The invention belongs to the field of preparation of functionalized polyethyleneimine materials, in particular to a pH sensitive zwitterion functionalized 99m Tc-labeled polyethyleneimine-wrapped nano-gold particle composite material and its preparation method. Background technique [0002] At present, cancer has become the number one killer that threatens human health. Due to the influence of external carcinogenic factors, the body undergoes mutations at the gene level, and local tissue cells lose control of their normal growth, resulting in local hyperplasia and tumors. Coupled with the characteristics of local invasion and distant metastasis of malignant tumors, it is more difficult to cure them. Therefore, timely diagnosis and treatment at the early stage of cancer can greatly reduce cancer mortality and improve the quality of life of patients. The development of molecular imaging technology provides the possibility for the early diagnosis of can...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/06C08G81/00A61K103/10
CPCA61K51/06C08G81/00
Inventor 朱静怡杨军星
Owner NANJING TECH UNIV