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Lignin and histidine drug-loaded nanoparticle with pH response and preparation method of lignin and histidine drug-loaded nanoparticle

A drug-loading nanometer and histidine technology, which is applied in the fields of biomedicine and polymer nanomaterials, can solve the problems of less application and research, and achieve the effects of reducing low toxicity, realizing intelligent controlled release, and improving drug stability.

Inactive Publication Date: 2018-10-16
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although alkali lignin is widely used in low-value-added industrial products as water reducers, adsorbents and additives, its application in high-value-added nanotechnology fields has been less studied

Method used

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  • Lignin and histidine drug-loaded nanoparticle with pH response and preparation method of lignin and histidine drug-loaded nanoparticle
  • Lignin and histidine drug-loaded nanoparticle with pH response and preparation method of lignin and histidine drug-loaded nanoparticle
  • Lignin and histidine drug-loaded nanoparticle with pH response and preparation method of lignin and histidine drug-loaded nanoparticle

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Amination of alkali lignin: Weigh 5g of alkali lignin, fully dissolve it in 50mL of water to form an aqueous solution of alkali lignin, add 6g of diethylenetriamine (DETA), adjust the pH to 12, and then slowly add 4.7mL of 37% formaldehyde dropwise solution. After the dropwise addition was completed, the temperature was raised to 60° C., and the reaction was carried out for 4 hours. After the reaction, adjust the acidity with 25% sulfuric acid to precipitate the aminated lignin, collect the precipitate after centrifugation, dialyze for 36 hours, and freeze-dry for 48 hours to obtain the aminated lignin.

[0022] Synthesis of lignin-histidine: Take 10 mg of aminated lignin, dissolve it in 10 mL of water, make it completely dissolved, add 7.12 mg of EDC and 4.28 mg of NHS, mix well, add 5.76 mg of histidine, stir magnetically, and keep at room temperature Under the reaction 3h. After the reaction, it was dialyzed in deionized water for 24 hours, and freeze-dried to obta...

Embodiment 2

[0025] Amination of alkali lignin: Weigh 3g of alkali lignin, fully dissolve it in 50mL of water to form an aqueous alkali lignin solution, add 3.6g of diethylenetriamine (DETA), adjust the pH to 12, and then slowly add 2.8mL of 37% formaldehyde solution. After the dropwise addition was completed, the temperature was raised to 60° C., and the reaction was carried out for 4 hours. After the reaction, adjust the acidity with 25% sulfuric acid to precipitate the aminated lignin, collect the precipitate after centrifugation, dialyze for 36 hours, and freeze-dry for 48 hours to obtain the aminated lignin.

[0026] Synthesis of lignin-histidine: Take 6 mg of aminated lignin, dissolve it in 10 mL of water, make it completely dissolved, add 4.27 mg of EDC and 2.57 mg of NHS, mix well, add 3.46 mg of histidine, stir magnetically, and keep at room temperature Under the reaction 3h. After the reaction, it was dialyzed in deionized water for 24 hours, and freeze-dried to obtain the lign...

Embodiment 3

[0029] Amination of alkali lignin: Weigh 4g of alkali lignin, fully dissolve it in 50mL of water to form an aqueous solution of alkali lignin, add 4.8g of diethylenetriamine (DETA), adjust the pH to 12, and then slowly add 3.8mL of 37% formaldehyde solution. After the dropwise addition was completed, the temperature was raised to 60° C., and the reaction was carried out for 4 hours. After the reaction, adjust the acidity with 25% sulfuric acid to precipitate the aminated lignin, collect the precipitate after centrifugation, dialyze for 36 hours, and freeze-dry for 48 hours to obtain the aminated lignin.

[0030] Synthesis of lignin-histidine: take 4 mg of aminated lignin, dissolve it in 10 mL of water, make it completely dissolved, add 2.85 mg of EDC and 1.71 mg of NHS, mix well, add 2.31 mg of histidine, stir magnetically, and keep at room temperature Under the reaction 3h. After the reaction, it was dialyzed in deionized water for 24 hours, and freeze-dried to obtain the l...

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Abstract

The invention discloses a lignin and histidine drug-loaded nanoparticle with pH response and a preparation method of lignin and the histidine drug-loaded nanoparticle. The lignin and histidine drug-loaded nanoparticle is characterized in that a lignin and histidine comjugate is formed by chemically ligating imidized lignin with histidine by amido bonds; hydroxyls in histidine and lignin moleculesare used as hydrophilic ends; a benzene ring in a lignin structure is used as a hydrophobic end; the lignin and the histidine conjugate is self-assembled in an aqueous solution to entrap 10-hydroxycamptothecin to further form the drug-loaded nanoparticle.

Description

technical field [0001] The invention relates to a pH-responsive lignin-histidine drug-loaded nanoparticle regulated by histidine and a preparation method thereof, belonging to the technical fields of biomedicine and polymer nanomaterials. Background technique [0002] In recent years, with the continuous research on nano-drug carriers, smart nano-drug carriers have become a research hotspot. Intelligent nano-drug carrier refers to the use of special structures or molecules, through artificial design, synthesis can recognize the microenvironment, and under the stimulation of specific environmental, physical or chemical factors, rapidly release drugs through changes in carrier structure, configuration and other characteristics new carrier. In addition to enhancing the water solubility of drugs, prolonging their systemic circulation time, improving their bioavailability, smart nano-drug carriers can overcome biological barriers, adjust drug distribution in the body, and improv...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/30A61K47/22A61K31/4745A61P35/00
CPCA61K9/5123A61K9/513A61K31/4745A61P35/00
Inventor 雷建都赵静养陶英华王璐莹刘静何静
Owner BEIJING FORESTRY UNIVERSITY
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