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Method for synthesizing polyvinyl alcohol embolization microspheres capable of loading chemotherapeutic drug epirubicin

A polyvinyl alcohol embolic microsphere and epirubicin technology, which is applied in the field of medical materials, can solve problems such as embolization errors, catheter blockage, tissue damage, etc., and achieve the effects of simple method process, increased drug loading, and smooth surface

Inactive Publication Date: 2018-07-03
SUZHOU HENGRUI CALLISYN BIOLOGICAL MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The key to minimally invasive interventional therapy is to select the appropriate embolic agent for blocking blood supply to the tissue. The physical characteristics of the embolic agent are crucial to the final efficacy of the interventional therapy. Embolic agent products can lead to the following problems in interventional surgery: (1) blockage of the catheter; (2) misembolization, that is, the embolization point is too far away from the tumor tissue, causing damage to normal tissue; Then leave the predetermined embolization position and enter other blood vessels; (4) The target blood vessel cannot be completely embolized
However, the chemotherapy drug infusion method currently used in clinical practice cannot fully guarantee the local drug release of chemotherapy drugs due to the limitation of embolic agents.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Add 150 g of polyvinyl alcohol into a flask filled with pure water, stir and disperse evenly. Heat up to 96°C, after the polyvinyl alcohol is completely dissolved, cool down to 10-15°C, add 3.0g of intermediate acrylamidoalkyldialkoxy acetal, N-acrylamidodimethoxy After stirring for 10 minutes, 100ml of concentrated hydrochloric acid was added dropwise to the solution. After the dropwise addition, the reaction continued to stir for 6 hours, and then the crude product was collected, washed and dried to obtain the desired functionalized macromolecular hydrogel Glue (referred to as Calli-B).

Embodiment 2

[0021] Add 15 g of sodium 2-acrylamide-2-methylpropanesulfonate and 10 g of potassium persulfate into water in sequence, dissolve and mix evenly, then add the functionalized macromolecular gel intermediate (Calli-B) prepared in Example 1 100.00 g and stir evenly to obtain a polymer monomer solution. Add 10 g of butyl acetate and 5 g of cellulose acetate into the reaction vessel, and feed N at the same time. 2 Gas, stirring, heating, and then sequentially add the above-mentioned polymer monomer solution and tetramethylethylenediamine to form an oil-water mixed reaction system, heating and stirring for 3 hours. In this reaction, the stirring paddle is an axial-flow stirring paddle, the stirring speed is controlled at 400 rpm, and the temperature of the reaction system is controlled at 40-50° C. when the polymer monomer solution is added. After the reaction is finished, the reaction mixture is filtered to collect the microspheres, washed with butyl acetate, ethyl acetate and ace...

Embodiment 3

[0023] Dissolve 10mg of epirubicin in 2.0ml of pure water, take the microsphere embolism synthesized in Example 2, accurately weigh 0.25g, put it into a 20ml vial, add 2ml of the above-mentioned epirubicin solution, and make The microspheres were soaked in the epirubicin solution, and the mixture was shaken occasionally. Use a micro-syringe to regularly sample 20 μL at the 5th, 10th, 20th, 40th, and 60th minute, add 5.0ml of pure water to dilute, measure the absorbance at 485nm, and substitute the absorbance into the standard curve equation to calculate the concentration of the drug contained in the sample. The drug loading amount of the ball to epirubicin: drug loading=(drug content in the solution before drug loading-drug content in the solution after drug loading) / microsphere weight. The microsphere-loaded epirubicin drug load was measured to be 38mg / gram of microsphere.

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Abstract

The invention relates to a method for synthesizing polyvinyl alcohol embolization microspheres capable of loading a chemotherapeutic drug epirubicin. According to the present invention, by researchingthe formula and the synthesis process of the synthesis reaction, the epirubicin loading of the polyvinyl alcohol embolization microspheres is increased; the technical scheme comprises that polyvinylalcohol is completely dissolved, the dissolved polyvinyl alcohol is cooled to a temperature of 10-15 DEG C, a ratio of Calli-B to 2-acrylamide-2-methyl propyl sodium sulfonate is 1.00:0.15, an axial flow type stirring paddle is selected, the stirring speed is controlled at 400 rpm, and the temperature of the reaction system is controlled at 40-50 DEG C when a polymer monomer solution is added; andby researching the formula, the stirring mode, the stirring speed and the reaction temperature of the synthesis reaction, the problem of the low epirubicin loading of the polyvinyl alcohol embolization microspheres is solved, the epirubicin loading of the polyvinyl alcohol embolization microspheres is increased, and the drug-loading microspheres can continuously release epirubicin to the targeting tumor area at the tumor site.

Description

technical field [0001] The invention relates to a method for synthesizing polyvinyl alcohol embolism microspheres capable of loading chemotherapeutic drug epirubicin, and belongs to the technical field of medical materials. Background technique [0002] Minimally invasive interventional therapy is becoming more and more widely used in the field of medical technology, especially in the treatment of cancer tumors rich in blood vessels such as liver cancer, kidney cancer, and uterine fibroids, and has become an important tool for the treatment of tumors that cannot be surgically removed. preferred alternative to . The principle is to use high-definition medical imaging equipment to guide the catheter through the artery to the tumor site in the human body, and then infuse the embolism agent of anti-tumor drugs through the catheter to block the blood supply of the tumor tissue, so that the tumor shrinks in a short time. Therapeutic purposes of necrosis. The key to minimally inv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61L24/06A61K9/16A61K47/32A61K31/704A61P35/00
CPCA61L24/06A61K9/1635A61K31/704A61L24/001A61L24/0015A61L2300/416A61L2300/60C08L51/003
Inventor 郁娅卿
Owner SUZHOU HENGRUI CALLISYN BIOLOGICAL MEDICINE TECH CO LTD
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