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Targeting carrier material and targeting micelle preparation of liver tumors and preparation methods thereof

A carrier material and liver tumor technology, which is applied in the direction of anti-tumor drugs, pharmaceutical formulations, medical preparations with non-active ingredients, etc., can solve the problem that anti-liver tumor drugs cannot accurately select tumor cells, etc. Good sealing rate and suitable potential

Active Publication Date: 2018-11-30
YANTAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The first purpose of the present invention is to provide a liver tumor targeting carrier material, which has reduction sensitivity and can realize targeted selection for tumor microenvironments with high reducing substances, and solves the problem of anti-liver tumor drugs in the prior art. Technical problems of inability to accurately select tumor cells

Method used

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  • Targeting carrier material and targeting micelle preparation of liver tumors and preparation methods thereof
  • Targeting carrier material and targeting micelle preparation of liver tumors and preparation methods thereof
  • Targeting carrier material and targeting micelle preparation of liver tumors and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] This example provides a method for preparing a liver tumor targeting carrier material, the steps are as follows:

[0084] 1. Synthesis of A

[0085]

[0086] (1) Weigh 0.020g of APS into the EP tube, add 2mL of DMF, and dissolve the APS completely by heating in a water bath or ultrasonic method; wherein, the APS is pretreated as follows: the APS is separated by dialysis and G50 glucose gel column Purify to obtain refined angelica polysaccharide with a sugar content of 92% and a molecular weight of about 10,000 Da;

[0087] (2) Weigh 0.020g of EDC and 0.015g of DMAP into an EP tube, add 3mL of DMF to dissolve it, combine the solution prepared in step (1) and step (2), seal it, and activate it at 55°C for 30min;

[0088] (3) Weigh 0.047g of GA into the EP tube, add 2mL of DMF, and dissolve the GA completely by heating in a water bath or ultrasonic method; slowly add the GA dissolved in DMF into the step (2) under stirring condition for activation In the solution, aft...

Embodiment 2

[0104] This embodiment refers to the preparation method of Example 1, the difference is only that in the preparation process of A, the mass ratio of APS, EDC and DMAP is 1:1.2:1, the mass ratio of APS and GA is 1:4, and the steps ( 3) The middle reaction temperature is 45°C.

Embodiment 3

[0106] This example refers to the preparation method of Example 1, the only difference is that in the preparation process of compound C, the molar ratio of 3,3-dithiodipropionic acid to oxalyl chloride is 1:2, and the reaction temperature of the two is 40 ℃, the reaction temperature of curcumin and compound B is 30 ℃.

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Abstract

The invention relates to the technical field of targeted drug carriers and preparations, in particular to a targeting carrier material and a targeting micelle preparation of liver tumors and preparation methods thereof. The targeting carrier material of the liver tumors is mainly formed by sequentially and covalently connecting angelica polysaccharide, glycyrrhetinic acid and antitumor drugs for the liver tumors, wherein the glycyrrhetinic acid and the antitumor drugs for the liver tumors are covalently connected through disulfide bonds. The micelle preparation comprises the targeting carriermaterial of the liver tumors and the antitumor drugs for the liver tumors, and the antitumor drugs for the liver tumors are encapsulated in the targeting carrier material of the liver tumors. The carrier material has reduction sensitivity, and can realize targeting selection on a tumor microenvironment with high reducing substances; the micelle preparation is formed by self-assembly of the carriermaterial and the antitumor drugs for the liver tumors; and the solubility and stability of hydrophobic drugs are enhanced by utilizing the characteristics of polymer-drug conjugates of the carrier material, and drug release can be carried out under the reduction environment.

Description

technical field [0001] The invention relates to the technical field of targeting drug carriers and preparations, in particular to a liver tumor targeting carrier material, a micelle preparation and a preparation method thereof. Background technique [0002] In recent years, tumors have caused great harm to people's health and have many complications. According to research and investigation in recent years, the death rate caused by tumors ranks second among all diseases, second only to cardiovascular and cerebrovascular diseases. Among them, the incidence of liver tumors in our country is very high. With the acceleration of the aging process of our country, the incidence of liver tumors is increasing day by day, and the treatment and prevention of liver tumors are getting more and more attention. [0003] At this stage, the treatment measures for liver tumors mainly include surgery, radiation and drug therapy, and drug therapy is still the main treatment. After traditional ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/55A61K47/61A61K31/56A61P35/00A61K31/12
CPCA61K9/1075A61K31/12A61K31/56A61K47/55A61K47/61A61P35/00A61K2300/00
Inventor 陈大全王炳杰房蕾王凯丽刘梦娜范辛辛
Owner YANTAI UNIV
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