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Multiple sustained release vascular embolization drug-loading composition

A technology of vascular embolism and composition, which is applied in the field of multiple slow-release vascular embolism drug-loaded compositions, which can solve problems such as adverse reactions, affecting long-term therapeutic effect, and increased drug concentration, and achieve the effect of drug burst release

Active Publication Date: 2019-06-04
太阳雨林(厦门)生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the prior art, drug-loaded microspheres sometimes experience sudden drug release during the treatment process, resulting in a sudden increase in the drug concentration in the body, resulting in serious adverse reactions, and affecting the long-term therapeutic effect

Method used

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  • Multiple sustained release vascular embolization drug-loading composition
  • Multiple sustained release vascular embolization drug-loading composition
  • Multiple sustained release vascular embolization drug-loading composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] A drug-loaded composition for multiple sustained-release vascular embolism, the drug is released from it in 1-360 days, and the degradation time in vivo is 1-360 days, which includes drug-loaded microspheres and is made of degradable and / or non-degradable materials A three-dimensional porous scaffold, the drug-loaded microspheres are loaded in the three-dimensional porous scaffold through hydrogel or autologous blood clot, so that the drug in the drug-loaded microspheres is released from the drug-loaded microspheres to the hydrogel or autologous blood clot, and then It is then released into the three-dimensional porous scaffold, and finally released outside the three-dimensional porous scaffold. The pores of the three-dimensional porous scaffold are evenly distributed, and the pore diameter of the pores is larger than the diameter of the drug-loaded microspheres, wherein the diameter of the drug-loaded microspheres is 5nm-900μm, and the pore diameter of the pores of the ...

Embodiment 2

[0050] (1) Preparation of degradable drug-loaded microspheres (taking chitosan and gelatin microspheres as examples): after dissolving the gelatin solution / chitosan solution with a concentration of 10% on a water bath at 50-60° C. Add doxorubicin hydrochloride and mix thoroughly in a vortex mixer to make an aqueous phase. Add an appropriate amount of Span-80 to liquid paraffin to form the oil phase, place it in a three-necked bottle in a constant temperature water bath at 50°C, and stir at a speed of 200-1000r·min -1 Under certain conditions, slowly emulsify the water phase into the oil phase drop by drop, the ratio of water to oil is 1:4-1:8. Microscopic examination until the emulsion drops into a spherical shape of suitable size, that is, after emulsification to form a stable W / O emulsion, quickly cool down to below 5°C, add formaldehyde or 50% glutaraldehyde to cure for 1-2 hours, and the obtained product will be heated at 3000r / min Centrifuge, wash with isopropanol and ac...

Embodiment 3

[0054](1) Preparation of non-degradable drug-loaded microspheres (taking PVA microspheres as an example): under stirring conditions, add 2 g of surfactant Span-80 to 40 mL of liquid paraffin to form a continuous oil phase; , add 10mL of PVA to the oil phase, after mixing well, add 1g of STMP as a cross-linking agent, and immediately add 1mL of NaOH as a catalyst. Set the rotation speed to 400r / min, the temperature to 50°C, and the reaction time to 16h. After the cross-linking reaction is over, let it stand for 30 minutes. Add a small amount of absolute ethanol, put it in a centrifuge for centrifugation, take out the supernatant, wash the precipitate repeatedly with absolute ethanol, isopropanol and pure water, and finally put it in a blast drying oven for 24 hours to obtain White powder, its scanning electron microscope picture is as follows Figure 6 shown.

[0055] (2) Preparation of degradable three-dimensional porous scaffold (PCL porous scaffold as an example): PCL7g, ...

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Abstract

The present invention discloses a multiple sustained release vascular embolization drug-loading composition. Release time of drugs from the composition is 1-360 d, and the drug-loading composition comprises a drug-loading microsphere made of a degradable material and / or a non-degradable material and a three-dimensional porous scaffold made of a degradable material and / or a non-degradable material.The three-dimensional porous scaffold has a uniform pore distribution and besides a pore diameter of pores is larger than a diameter of the drug-loading microsphere; the drug-containing drug-loadingmicrospheres pass through hydrogels or autologous coagulated blood blocks loaded in the three-dimensional porous scaffold, so that the drugs in the drug-loading microspheres are released from the drug-loading microspheres to the hydrogels or autologous coagulated blood blocks, then released into the three-dimensional porous scaffold and finally released outside the three-dimensional porous scaffold; or drug-free drug-loading microspheres are loaded into the three-dimensional porous scaffold to form a complex, then the drugs are loaded into the complex, and the drugs are released from the complex to the outside of the three-dimensional porous scaffold. The multiple sustained release vascular embolization drug-loading composition effectively solves a problem of drug burst release of the drug-loading microspheres.

Description

technical field [0001] The invention belongs to the technical field of biomedical engineering, and in particular relates to a drug-loaded composition for multiple slow-release blood vessel embolism. Background technique [0002] New embolic agents are one of the research hotspots in recent years. Among them, drug-eluting microspheres (drug-eluting bead, DEB) are a potential application due to their embolization and drug-loading properties. Excellent clinical chemoembolization material. DEB adsorbs antitumor drugs (such as doxorubicin, epirubicin and daunorubicin, irinotecan, topotecan and sorafenib, etc.) through ion exchange, and can be simultaneously guided by a single image. Realize the arterial delivery of drugs and embolic agents, so that they can release chemotherapy drugs stably at the tumor site, so that the local tumor maintains a high blood drug concentration, while the systemic blood drug concentration is low, thereby reducing side effects. [0003] Drug-loaded ...

Claims

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Application Information

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IPC IPC(8): A61L24/00A61L24/08A61L24/10A61L24/04A61L24/06
Inventor 赵一麟周媛媛
Owner 太阳雨林(厦门)生物医药有限公司
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