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Drug carrying microsphere with tumor chemoradiotherapy synergistic sensitization effect and preparation method thereof

A technology of drug-loaded microspheres, radiotherapy and chemotherapy, which is applied in the field of nanomaterials, can solve the problems of limited anti-tumor effect of drugs, poor histocompatibility, and large drug dosage, and achieves excellent pH responsiveness, easy operation, and reaction. mild conditions

Active Publication Date: 2020-06-12
SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the drug-loaded nanoparticles still encounter many obstacles in the process of delivery to tumor cells, such as deep penetration into the tumor, drug transport, intracellular release, etc., resulting in a greatly limited anti-tumor effect of the drug. The effect of treatment often requires the injection of a large amount of drug-loaded nanoparticles, and the drug is released early and interacts with normal tissues before reaching the tumor tissue, resulting in premature drug failure
[0005] Therefore, the clinically used drugs for the treatment of liver cancer in related technologies still have problems such as large drug dosage, poor tissue compatibility, and failure of drugs due to early release.

Method used

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  • Drug carrying microsphere with tumor chemoradiotherapy synergistic sensitization effect and preparation method thereof
  • Drug carrying microsphere with tumor chemoradiotherapy synergistic sensitization effect and preparation method thereof
  • Drug carrying microsphere with tumor chemoradiotherapy synergistic sensitization effect and preparation method thereof

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preparation example Construction

[0074] refer to figure 1 , which shows a flow chart of an embodiment of a method for preparing drug-loaded microspheres with a synergistic sensitization effect of tumor radiotherapy and chemotherapy of the present invention, which may specifically include:

[0075] Step S41, polyacrylic acid PAA and polyethylene glycol PEG aminated at both ends are subjected to amide reaction under the action of the first activator to obtain a block polymer of PAA-PEG;

[0076] Step S42, the block polymer of PAA-PEG and 1-hydroxyethyl-2-methyl-5-nitroimidazole MN are subjected to an esterification reaction under the action of a second activator to obtain MN-PAA - PEG polymer microspheres;

[0077] In step S43, the MN-PAA-PEG polymer microspheres and doxorubicin DOX are self-assembled to obtain doxorubicin-loaded DOX / MN-PAA-PEG microspheres.

[0078] The drug-loaded microspheres with synergistic sensitization effect of tumor radiotherapy and chemotherapy provided by the embodiment of the pres...

Embodiment 1

[0093] The drug-loaded microspheres with synergistic sensitization effect of tumor radiotherapy and chemotherapy of the present invention are composed of polyacrylic acid PAA, polyethylene glycol PEG aminated at both ends, 1-hydroxyethyl-2-methyl-5-nitroimidazole MN And doxorubicin DOX is used as a raw material, and is prepared through amide reaction, esterification reaction and self-assembly.

[0094] This example discloses the preparation method of the drug-loaded microspheres with synergistic sensitization effect of tumor radiotherapy and chemotherapy of the present invention, specifically:

[0095] Step 1, polyacrylic acid PAA and polyethylene glycol PEG aminated at both ends, under the effect of the first activator, carry out amide reaction, obtain the block polymer of PAA-PEG:

[0096] Dissolve 300mg of polyacrylic acid PAA (number average molecular weight 2000) in 30mL of 2-(N-morpholino)-ethanesulfonic acid buffer (MES, 10Mm, pH 6.0) to form a homogeneous polyacrylic a...

Embodiment 2

[0111] Step 1. Dissolve 300mg of polyacrylic acid (PAA, number average molecular weight 2000) in 30mL of 2-(N-morpholino)-ethanesulfonic acid buffer (MES, 10Mm, pH 6.0) to form a polyacrylic acid solution , 57.5 mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and 34.5 mg of N-hydroxysuccinimide (NHS) were added to the PAA solution to obtain Mixture A was activated at room temperature for 10 min. Then use triethylamine (TEA) to adjust the pH value of the mixed solution to 7.2 to form the activated polyacrylic acid mixed solution B; Polyethylene glycol (PEG, number average molecular weight: 7000), stirred at room temperature for 16 hours to obtain a mixed solution containing PAA-PEG, dialyzed to remove impurities, and dried to obtain a PAA-PEG block polymer;

[0112] Step 2. Dissolve 300mg of PAA-PEG in 15mL of dimethyl sulfoxide, then add 123mg of EDC and 76mg of 4-dimethylaminopyridine (DMAP) in sequence, and stir for 2 hours in the dark to obtain a mi...

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Abstract

The invention provides a drug carrying microsphere with a tumor chemoradiotherapy synergistic sensitization effect and a preparation method thereof. The method comprises the following steps: carryingout amidation reaction on a polyacrylic acid PAA and polyethylene glycol PEG with two end amination under action of a first activating agent to obtain a PAA-PEG block polymer; carrying out esterification reaction on the PAA-PEG block polymer and 1-ethoxy-2-methyl-5-nitroimidazole MN under the action of a second activating agent to obtain a MN-PAA-PEG polymer microsphere; and carrying out self-assembly on the MN-PAA-PEG polymer and doxorubicin DOX to obtain a doxorubicin-loaded DOX / MN-PAA-PEG microsphere. The drug carrying microsphere can be obtained only through three steps of an acylation reaction, an esterification reaction and self-assembly, the method has characteristics of a simple process, mild reaction conditions and easiness in operation.

Description

technical field [0001] The invention relates to the technical field of nanomaterials, in particular to a drug-loaded microsphere with a synergistic sensitization effect of tumor radiotherapy and chemotherapy and a preparation method thereof. Background technique [0002] Cancer is one of the most lethal diseases in the world, and the global cancer incidence and mortality are increasing rapidly. According to the 2018 Global Cancer Annual Report, liver cancer is expected to become the sixth most common cancer and the fourth leading cause of cancer death worldwide in 2018. In 2018, there were 78,300 deaths from liver cancer worldwide, accounting for 8.2%. The mortality rate of liver cancer ranks fourth in the world and fifth in China. [0003] At present, the methods for clinical treatment of liver cancer mainly include surgical resection, radiotherapy and chemotherapy. Among them, systemic chemical drug therapy: For patients with advanced primary liver cancer, not only the p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K47/32A61K41/00A61K31/704A61P35/00
CPCA61K9/5138A61K9/5146A61K31/704A61K41/0038A61P35/00A61K2300/00
Inventor 黄忠兵翁佳佳尹光福
Owner SICHUAN UNIV
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