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Preparation method and application of a lignin-based antitumor drug carrier

An anti-tumor drug, a lignin-based technology is applied in the field of preparation of a lignin-based anti-tumor drug carrier, and can solve the problems of lack of pH response characteristics, low drug loading and encapsulation rate, inability to target drug release, and the like, Achieve sensitive pH response performance, significant economic and social benefits, and reduce toxic and side effects

Active Publication Date: 2022-05-17
HENAN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the above situation, in order to overcome the defects of the prior art, the purpose of the present invention is to provide a preparation method and application of a lignin-based anti-tumor drug carrier, which can effectively solve the complex preparation process of the lignin-based drug carrier, low efficiency, and drug loading. The amount and encapsulation efficiency are too low, there is no pH response characteristic, and the drug cannot be released in a targeted manner, so it is not suitable for the problem of encapsulating anti-tumor drugs

Method used

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  • Preparation method and application of a lignin-based antitumor drug carrier
  • Preparation method and application of a lignin-based antitumor drug carrier
  • Preparation method and application of a lignin-based antitumor drug carrier

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Embodiment 1

[0027] A preparation method of a lignin-based antitumor drug carrier of the present invention comprises the following steps:

[0028] (1) Preparation of carrier components: The carrier is composed of the following weights: 100 parts of alkali lignin, 35 parts of formaldehyde, 60 parts of sulfonating reagent, 60 parts of cationizing reagent, 40 parts of cationic surfactant, organic solvent 550 parts and 25 parts of antineoplastic drugs are formulated;

[0029] (2) Add water to alkali lignin to make a solution, adjust the pH to 11, heat up to 70°C, add formaldehyde, react for 3 hours to obtain hydroxymethylated lignin, then add sulfonating reagent, react for 2.5 hours to obtain sulfonamide Then add cationic reagents to react for 2 hours, transfer the reacted solution to a dialysis bag with a molecular weight cut-off of 2000 for dialysis and purification for 6 days (days), spin evaporate, and freeze-dry to obtain amphoteric lignin;

[0030] (3) Dissolve the amphoteric lignin in ...

Embodiment 2

[0033] A preparation method of a lignin-based antitumor drug carrier of the present invention comprises the following steps:

[0034] (1) Add water to 100 parts of aspirin lignin to make a solution, adjust the pH to 10, raise the temperature to 70°C, add 20 parts of formaldehyde, and react for 1.5 hours to obtain hydroxymethylated lignin, then add sulfonating reagent 20 parts of sodium bisulfite were reacted for 1 hour to obtain sulfomethylated lignin, and then 20 parts of cationization reagent 2,3-epoxypropyltrimethylammonium chloride were added to react for 4 hours, and the reacted solution was transferred to Purified by dialysis in a dialysis bag with a molecular weight cut-off of 1000 for 6 days, rotary steamed, and freeze-dried to obtain amphoteric lignin;

[0035] (2) Dissolve the amphoteric lignin in water, add a sodium hydroxide solution with a mass concentration of 20%, adjust the pH of the amphoteric lignin solution to 7, make the surface of the amphoteric lignin neg...

Embodiment 3

[0039]A preparation method of a lignin-based antitumor drug carrier of the present invention comprises the following steps:

[0040] (1) Add water to 100 parts of wheatgrass lignin to make a solution, adjust the pH to 9, raise the temperature to 60°C, add 30 parts of formaldehyde, and react for 3 hours to obtain hydroxymethylated lignin, then add 30 parts of concentrated sulfuric acid as a sulfonating agent Parts, reacted for 2 hours to obtain sulfomethylated lignin, then added 35 parts of cationic reagent N-dimethylazetidine chloride and reacted for 3 hours, and transferred the reacted solution to a dialysis bag with a molecular weight cut off of 2000 Purified by medium dialysis for 5 days, rotary steamed, and freeze-dried to obtain amphoteric lignin;

[0041] (2) Dissolve the amphoteric lignin in water, add a sodium carbonate solution with a mass concentration of 25%, adjust the pH of the amphoteric lignin solution to 8, make its surface negatively charged, and then add the ...

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Abstract

The invention relates to a preparation method and application of a lignin-based anti-tumor drug carrier, which can effectively solve the complex preparation process of the lignin-based drug carrier, low efficiency, low drug loading and encapsulation efficiency, no pH response characteristics, and inability to target The release of drugs is not suitable for the problem of carrying anti-tumor drugs. The technical solution is, by weight: 100 parts of alkali lignin, 20-50 parts of formaldehyde, 20-100 parts of sulfonating reagent, 20-100 parts of cationizing reagent 100 parts, 30-50 parts of cationic surfactant, 100-1000 parts of organic solvent and 1-50 parts of antineoplastic drug. It has good compatibility, effectively reduces the toxic and side effects of drugs on normal tissue cells, prevents the photolysis and oxidation of drugs, and improves the utilization rate and efficacy of drugs. It is an innovation in the preparation of oral anti-tumor drug carriers and anti-tumor drugs. economic and social benefits.

Description

technical field [0001] The invention relates to medicine, in particular to a preparation method and application of a lignin-based antitumor drug carrier. Background technique [0002] Cancer is currently a major cause of human death. Chemotherapy plays an important role in the treatment of cancer. However, most drugs have problems such as poor water solubility, poor distribution in the body, and large toxic and side effects, which greatly limit the anti-tumor effect. Because the metabolic rate of tumor cells is faster than that of normal tissues, a large amount of acidic metabolites accumulate in the extracellular matrix of tumor cells, resulting in a low local pH of the tissues around tumor cells. The pH value of normal human tissues is 7.4, while the pH value of tumor cell lysosomes is about 5.0. The biodistribution of anti-tumor drugs can be changed through the pH-responsive drug delivery system, the anti-tumor efficiency can be improved, and the toxic and side effects o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/30A61K31/704A61K31/337A61K31/12A61P35/00
CPCA61K9/1629A61K9/1682A61K31/704A61K31/337A61K31/12A61P35/00
Inventor 李圆圆王斯佳李朋伟张景亚于丁一
Owner HENAN UNIV OF CHINESE MEDICINE