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Traditional Chinese medicine composite temperature-sensitive gel embolization agent, and preparation method and application thereof

A sensitive gel embolism, traditional Chinese medicine technology, applied in the field of anti-tumor preparations, can solve the problems of poor oral absorption, insoluble in water, low bioavailability, etc., and achieve the effect of good fluidity and good MRI visualization function

Active Publication Date: 2022-02-25
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of these compounds are insoluble in water, have poor oral absorption and low bioavailability

Method used

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  • Traditional Chinese medicine composite temperature-sensitive gel embolization agent, and preparation method and application thereof
  • Traditional Chinese medicine composite temperature-sensitive gel embolization agent, and preparation method and application thereof
  • Traditional Chinese medicine composite temperature-sensitive gel embolization agent, and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] (1) Preparation and characterization of superparamagnetic iron oxide nanoparticles: Weigh 0.27g FeCl 3 •6H 2 O, 0.75g sodium acrylate, 0.75g anhydrous sodium acetate in a round bottom flask, add 10mL diethylene glycol, mechanically stir for 24h, transfer to a high pressure reactor, react at 190°C for 10h, after natural cooling, 10mL Washing with absolute ethanol and centrifugation were repeated three times, and finally vacuum-dried to obtain superparamagnetic iron oxide nanoparticles. The particle size, potential and PDI of the prepared superparamagnetic iron oxide nanoparticles were measured by Malvern particle size analyzer, the morphology of superparamagnetic iron oxide nanoparticles was observed by scanning electron microscope, the iron content was determined by spectrophotometry, and magnetic resonance imaging The imaging performance of superparamagnetic iron oxide nanoparticles was measured by an instrument.

[0067] Such as Figure 1~3 As shown, the particle s...

Embodiment 2

[0109] Inhibits HIF-1 α Effects of expressed traditional Chinese medicine components on HepG2 cells in hypoxic state:

[0110] with CoCl 2 (200μM, 24h) induced HepG2 cells in a hypoxic state as a cell model, and Western blot was used to compare the effects of different concentrations (5, 10, 20, 40μM) of icariin on HIF-1 in liver cancer cells. α expressive influence. Such as Figure 16 As shown, with the increase of icariin concentration, its effect on HIF-1 in HepG2 cells under hypoxia α Increased inhibition of expression.

Embodiment 3

[0112] Add 250mg of ethyl oleate-tributyrin (mass ratio 1:1) to 600mg of surfactant HS-15, then take 160mg of co-surfactant PEG-400 into the above mixed system, and then take 17mg of Add mariin into the mixed system prepared above, stir magnetically for 2 hours, until no insoluble matter is suspended in the system, and set aside; finally, add 10 mL of 0.1 mg / mL deionized aqueous solution of superparamagnetic iron oxide nanoparticles at a constant speed, slowly and quantitatively dropwise into the above-prepared mixing system, and continuously stir the system at a constant speed until a transparent and clear system appears, which is the icariin magnetic microemulsion.

[0113] The ginseng polysaccharide was added into water, and magnetically stirred at 50° C. for 24 hours to obtain a polysaccharide aqueous solution. Take 140 mL of polysaccharide aqueous solution with a concentration of 20 mg / mL in a three-necked bottle; add 1.4 g of N -Isopropyl acrylamide, magnetic stirring f...

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Abstract

The invention relates to a traditional Chinese medicine composite temperature-sensitive gel embolization agent, and a preparation method and application thereof. The traditional Chinese medicine composite temperature-sensitive gel embolization agent comprises a traditional Chinese medicine polysaccharide composite temperature-sensitive material, superparamagnetic iron oxide nanoparticles, a traditional Chinese medicine component for inhibiting the expression of hypoxia-inducible factor-1 alpha (HIF-1 alpha), a mixed oil phase of triglyceride and ethyl oleate, a surfactant, a cosurfactant and water, wherein the traditional Chinese medicine polysaccharide composite temperature-sensitive material is a hydrogel material obtained by carrying out polymerization reaction on N-isopropylacrylamide in a traditional Chinese medicine polysaccharide solution. The traditional Chinese medicine composite temperature-sensitive gel embolism agent can significantly enhance the liver cancer vascular terminal embolism effect of the embolism agent, promote thrombosis of embolism parts, remodel a tumor immune microenvironment by inducing M1 type polarization of tumor-related macrophages (TAMs) and expression of HIF-1alpha, improve the curative effect of liver cancer interventional therapy and reduce the recurrence risk.

Description

technical field [0001] The invention belongs to the field of antitumor preparations, and in particular relates to a traditional Chinese medicine composite temperature-sensitive gel embolic agent, a preparation method of the temperature-sensitive gel embolic agent and an application in preparing an embolism therapeutic agent for liver cancer. Background technique [0002] Transarterial embolization / chemoembolization (TAE / TACE) is the clinical standard treatment method for advanced primary liver cancer. It can block the tumor blood supply by injecting embolization agents through the hepatic artery, resulting in ischemic necrosis. At present, TAE / TACE treatment still has the limitations of limited curative effect and easy recurrence. The important reasons are: ① The existing embolic agents cannot completely block the blood vessels at the end of the tumor, which will lead to the generation of collateral circulation and regain blood supply to the tumor site; ②Long-term ischemia a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L24/08A61L24/04A61L24/00A61L24/06A61L24/02A61K31/352A61K31/715A61K9/06A61K47/10A61K47/32A61K47/02A61P35/00A61P35/04A61K49/12
CPCA61L24/08A61L24/046A61L24/0015A61L24/06A61L24/02A61L24/0031A61L24/001A61K31/352A61K31/715A61K9/06A61K47/10A61K47/32A61K47/02A61P35/00A61P35/04A61K49/126A61L2300/416A61L2400/12A61L2300/216A61L2300/602C08L33/24C08L71/02C08L5/00A61K2300/00
Inventor 陈彦史新萌瞿鼎刘聪燕刘玉萍
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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