Folic acid modified gold nanoparticle, preparation method thereof, and applications of folic acid modified gold nanoparticle in preparation of radiosensitization therapy medicines

A technology of gold nanoparticles and radiation sensitization, which can be used in drug combinations, medical preparations of non-active ingredients, anti-tumor drugs, etc., and can solve problems such as complex synthesis of light-responsive molecules

Active Publication Date: 2018-09-28
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In fact, in vitro studies of light-triggered self-assembly of gold nanoparticles using photoresponsive molecules, such as isomerization or dimerization of chromophores, spiropyrans, azobenzenes, etc., have been reported; however, in None of the above studies have been applicable in vivo, and the synthesis of the light-responsive molecules involved is complex

Method used

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  • Folic acid modified gold nanoparticle, preparation method thereof, and applications of folic acid modified gold nanoparticle in preparation of radiosensitization therapy medicines
  • Folic acid modified gold nanoparticle, preparation method thereof, and applications of folic acid modified gold nanoparticle in preparation of radiosensitization therapy medicines
  • Folic acid modified gold nanoparticle, preparation method thereof, and applications of folic acid modified gold nanoparticle in preparation of radiosensitization therapy medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Add 1% chloroauric acid solution (0.6 mL) to ultrapure water (100 mL), heat to 100°C, stir vigorously until boiling, then add 1% sodium citrate solution (3 mL), wait until the system turns into wine After turning red, continue to boil for 30 min to obtain the stock solution of gold nanoparticles.

[0059] Add M-PEG sequentially to the gold nanoparticle stock solution (100 mL, containing 1 mg gold nanoparticles) 5000 -SH (20mg) and NH 2 -PEG 5000 -SH (20 mg), stirred at room temperature for 24h. After ultrafiltration and centrifugation (5000 rpm × 10 min) 5 times, excess PEG was removed. After centrifugation, resuspend with ultrapure water to obtain the mother solution of PEG-modified amino-functionalized gold nanoparticles.

[0060] UV-sensitive cross-linking agent (2.7 mg) and triethylamine ( 2.4 mg), stirred at room temperature for 4 h. After ultrafiltration and centrifugation (5000 rpm × 10 min) for 3 times, gold nanoparticles modified with UV-sensitive cross-l...

Embodiment 2

[0066] The folic acid-modified gold nanoparticles prepared in Example 1 were resuspended with ultrapure water, and placed in an ultraviolet lamp (405 nm, 1 W / cm 2 ) under irradiation for 10 min, the cross-linking of gold nanoparticles can be induced, and the folic acid-modified gold nanoparticle cross-linking body can be obtained.

[0067] Schematic diagram of the cross-linking agent at the PEG terminal on the surface of nanoparticles and the modification process of folic acid and the cross-linking process of nanoparticles triggered by ultraviolet light. figure 1 shown.

Embodiment 3

[0068] Example 3 Changes in hydrated particle size distribution and UV absorption of gold nanoparticles before and after crosslinking and TEM images

[0069] Dilute 100 μL (2 mg / mL) of the folic acid-modified gold nanoparticle aqueous solution (mother solution) and the folic acid-modified gold nanoparticle cross-linked product aqueous solution (mother solution) to 2 mL respectively, and test the particle size distribution (DLS) and UV absorption.

[0070] Such as figure 2 As shown in a, the hydrated particle size distribution of folic acid-modified gold nanoparticles is relatively uniform (about 60 nm), and the folic acid-modified gold nanoparticles irradiated by ultraviolet laser (405 nm, 25 min) can undergo cross-linking and aggregation, and the hydrated particles The diameter is about 300 nm.

[0071] figure 2 b is the UV absorption change of AuNPs after light-triggered cross-linking aggregation. The maximum absorption of folic acid-modified gold nanoparticles without...

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Abstract

The invention discloses folic acid modified gold nanoparticle, a preparation method thereof, and applications of the folic acid modified gold nanoparticle in preparation of radiosensitization therapymedicines. The preparation method comprises following steps: 1, the surfaces of nanoparticles are modified with an ultraviolet light sensitive cross-linking agent and folic acid; 2, ultraviolet lighttriggered gold nanoparticle crosslinking is carried out; and 3, ultraviolet light triggered nanoparticle application and radiosensitization are carried out. According to the preparation method, the crosslinking agent of a relatively small size is adopted, and nanoparticle precipitation is avoided; modification of tumor targeting functional molecules is carried out, so that the enrichment amount ofnanometer materials at tumor parts is increased effectively; ultraviolet light irradiation is adopted to realize controllable crosslinking of nanoparticle, and prolonging the detention time of nanometer materials at tumor parts greatly. The light triggered gold nanoparticle crosslinked product obtained using the preparation method is capable of enhancing tumor CT imaging and tumor radiosensitization therapy effect greatly, is suitable to be developed into an anti-tumor medicine based on radiosensitization therapy, and possesses high scientific research and economical value.

Description

technical field [0001] The invention belongs to the technical field of nanoparticle self-assembly, and specifically relates to a preparation method of a nanoparticle crosslinking strategy with tumor targeting function and ultraviolet light triggering, a crosslinked body prepared by the method, and the crosslinking strategy in the preparation of a nanoparticle based on The application of radiotherapy (Radiotherapy, RT) anti-tumor drugs. Background technique [0002] Malignant tumors have always been one of the major diseases that threaten human health, and their high morbidity and mortality have caused a heavy burden on human life and social economy for many years. How to realize the timely diagnosis and effective treatment of tumors has always been a major topic of concern to the medical community and scientists. [0003] It is well known that the small size and high specific surface area of ​​nanomaterials allow them to be passively enriched in tumor sites through the enha...

Claims

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Application Information

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IPC IPC(8): A61K33/24A61K9/14A61K47/22A61K49/04A61P35/00
CPCA61K9/145A61K33/24A61K49/04A61P35/00
Inventor 史海斌高明远程侠菊孙瑞
Owner SUZHOU UNIV
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