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PEG nuclear-crosslinked star high-molecular nano contrast agent and preparation method and application thereof

A nano-contrast agent and polymer technology, which is applied in the direction of medical preparations, pharmaceutical formulas, and preparations for in vivo tests with non-active ingredients, to achieve the effects of reducing toxicity or sensitization, reducing side effects, and maintaining contrast effects

Active Publication Date: 2019-10-25
SHANGHAI TENTH PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, there is no report about the PEG nuclear cross-linked star-shaped polymer nano-contrast agent used for fundus angiography of the present invention.

Method used

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  • PEG nuclear-crosslinked star high-molecular nano contrast agent and preparation method and application thereof
  • PEG nuclear-crosslinked star high-molecular nano contrast agent and preparation method and application thereof
  • PEG nuclear-crosslinked star high-molecular nano contrast agent and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 Preparation of PEG core cross-linked star-shaped polymer nano-contrast agent

[0040] 1. Materials

[0041] Polyethylene glycol methyl ether methacrylate (PPEGMA, M n =300), Sigma-Aldrich, Cat. No.: 447935; 2-cyano-2-propyl dodecyl trithiocarbonate (CTA), Sigma-Aldrich, Cat. No.: 723037; 1,4-dioxane, Sinopharm, product number: 10008918; 2,2′-Azobis(2-methylpropionitrile) (AIBN, CP), Aladdin, product number: A104256; 2,2′-Azobis(2-methylpropionitrile) Amidine) dihydrochloride (V-50, 97%), Sigma-Aldrich, Cat. No.: 440914; N,N'-bis(acryloyl)cystamine (BAC, 98%), Alfa Aesar, Cat. No.: A-4929 . BN rats were purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.; ICR mice were purchased from Shanghai Slack Experimental Animals Co., Ltd.; human retinal pigment epithelial cell line ARPE-19 was purchased from iCell Bioscience; human umbilical vein endothelial cells Purchased from Sciencell Company; ICG amine was purchased from AAT Bioquest, c...

Embodiment 2

[0058] Example 2S-PPEGMA 10 -Verification of the safety and effectiveness of ICG at the cell and animal levels

[0059] 1. Materials and methods

[0060] 1.1 CCK8 experiment

[0061] ARPE-19 and HUVEC cells in the logarithmic growth phase were taken, 5000 cells / well were spread into 96-well plates, and cultured in an incubator for 24 hours until the cells adhered to the wall. Add 0-400nmol / l ICG and S-PPEGMA respectively 10 -ICG, incubated for 24h. Change the medium, add 110uL of medium containing 10uL of CCK-8 to each well, and incubate for 2h in a 37°C incubator in the dark. For detection on the machine, a wavelength of 450nm is selected, and the OD value of each well is detected on a multi-functional microplate reader.

[0062] 1.2 Flow cytometry

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Abstract

The invention relates to a PEG nuclear-crosslinked star high-molecular nano contrast agent which is a star polymer having a PEG core prepared by bonding fluorescent groups. The invention also relatesto application of the PEG nuclear-crosslinked star high-molecular nano contrast agent in the preparation of fundal vascular contrast media. Part of patients intravenously injected with fundal vascularcontrast media clinically applied at present, such as sodium fluorescein or indocyanine green, experience adverse effects; these patients cannot take complete contrast examination. Compared with theprior contrast media, S-PPEGMA10-ICG herein has the advantages of low injection concentration and better choroidal development clarity; the side effects of prior drugs can be alleviated by lowering the administration concentration. In addition, successful construction of S-PPEGMA10-ICG also provides another choice for patients which experience allergy or other adverse effects when injected with existing contrast media, and therefore, the patients can gain diagnosis and treatment in time.

Description

technical field [0001] The invention relates to the technical field of fundus angiography, in particular to a PEG core-crosslinked star-shaped polymer nano-contrast agent and a preparation method and application thereof. Background technique [0002] Age-related macular degeneration (AMD) is one of the most important causes of central vision loss and irreversible blindness in the elderly over 50 years old. Currently, there are about 21 million AMD patients worldwide. AMD is divided into dry and wet types according to the presence or absence of neovascularization. Early dry AMD manifests as drusen, which does not seriously affect vision. In the late stage, geographic atrophy, discoid degeneration, etc. will appear, leading to vision loss. In wet AMD, due to the appearance of choroidal neovascularization (CNV) in the macular area, macular hemorrhage, edema, and severe vision loss are caused. Currently, the diagnostic methods for AMD include: fundus photography, OCT, and fund...

Claims

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Application Information

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IPC IPC(8): A61K49/00A61K47/60
CPCA61K49/0034A61K49/0043A61K49/0054
Inventor 于靖赵鹏蔡雯婷陈起静范佳淇
Owner SHANGHAI TENTH PEOPLES HOSPITAL
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