Targeted folic acid-polyethylene glycol-lignin conjugate medicine-carrying nano particles and preparation method thereof

A technology of polyethylene glycol and drug-loaded nanometers, which is applied in the fields of biomedicine and nanomedicine

Inactive Publication Date: 2018-09-28
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, lignin-based drug-loaded nanoparticles with both active targeting and long circulation in vivo have not been reported

Method used

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  • Targeted folic acid-polyethylene glycol-lignin conjugate medicine-carrying nano particles and preparation method thereof
  • Targeted folic acid-polyethylene glycol-lignin conjugate medicine-carrying nano particles and preparation method thereof
  • Targeted folic acid-polyethylene glycol-lignin conjugate medicine-carrying nano particles and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0022] (1) Synthesis of folic acid-polyethylene glycol conjugate: Weigh 440 mg of folic acid and dissolve it in 15 mL of anhydrous DMSO; after fully dissolving, add EDC (380 mg) and NHS (345 mg) and activate for 15 min; add polyethylene glycol ( 2.0 g), stirred and reacted at room temperature for 24 hours; after the reaction was completed, dialyzed with pure water for 3 hours, and freeze-dried to obtain a solid folic acid-polyethylene glycol conjugate;

[0023] (2) Synthesis of folic acid-polyethylene glycol-lignin conjugate: Weigh 200 mg of purified alkali lignin, dissolve it in 15 mL of tetrahydrofuran, add 400 mg of folic acid-polyethylene glycol conjugate; after fully dissolving, add EDC (190mg) and DMAP (180mg), stirred and reacted for 24 hours; after the reaction was completed, the reaction solution was dropped into anhydrous ether to precipitate a precipitate; Reagents and organic solvents, freeze-dried to obtain folic acid-polyethylene glycol-lignin conjugates with hig...

Embodiment 2

[0026] (1) Synthesis of folic acid-polyethylene glycol conjugate: Weigh 440 mg of folic acid and dissolve it in 15 mL of anhydrous DMSO; after fully dissolving, add EDC (380 mg) and NHS (345 mg) and activate for 15 min; add polyethylene glycol ( 2.0 g), stirred and reacted at room temperature for 24 hours; after the reaction was completed, dialyzed with pure water for 3 hours, and freeze-dried to obtain a solid folic acid-polyethylene glycol conjugate;

[0027] (2) Synthesis of folic acid-polyethylene glycol-lignin conjugate: Weigh 200 mg of purified alkali lignin, dissolve it in 15 mL of tetrahydrofuran, add 300 mg of folic acid-polyethylene glycol conjugate; after fully dissolving, add EDC (190mg) and DMAP (180mg), stirred and reacted for 24 hours; after the reaction was completed, the reaction solution was dropped into anhydrous ether to precipitate a precipitate; Reagents and organic solvents, freeze-dried to obtain folic acid-polyethylene glycol-lignin conjugates with hig...

Embodiment 3

[0030] (1) Synthesis of folic acid-polyethylene glycol conjugate: Weigh 440 mg of folic acid and dissolve it in 15 mL of anhydrous DMSO; after fully dissolving, add EDC (380 mg) and NHS (345 mg) and activate for 15 min; add polyethylene glycol ( 2.0 g), stirred and reacted at room temperature for 24 hours; after the reaction was completed, dialyzed with pure water for 3 hours, and freeze-dried to obtain a solid folic acid-polyethylene glycol conjugate;

[0031] (2) Synthesis of folic acid-polyethylene glycol-lignin conjugate: Weigh 200 mg of purified alkali lignin, dissolve it in 15 mL of tetrahydrofuran, add 500 mg of folic acid-polyethylene glycol conjugate; after fully dissolving, add EDC (340mg) and DMAP (250mg), stirred and reacted for 24h; after the reaction was completed, the reaction liquid was dropped into anhydrous ether to precipitate a precipitate; the precipitate was redissolved in 10mL pure water, and dialyzed in pure water for 6h to remove Reagents and organic s...

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Abstract

The invention discloses targeted folic acid-polyethylene glycol-lignin conjugate medicine-carrying nano particles and a preparation method thereof. The particles are characterized in that a folic acid-polyethylene glycol-lignin conjugate is formed by chemically connecting folic acid, amidogen-polyethylene glycol-carboxyl and lignin, lignin is used as a framework material, amidogen-polyethylene glycol-carboxyl is used as a connection arm, folic acid is used as a targeted molecule, and the folic acid-polyethylene glycol-lignin conjugate is self-assembled in an aqueous solution and wraps 10-hydroxycamptothecin to form the targeted medicine-carrying nano particles. According to the medicine-carrying nano particles, the solubility, the stability, the permeability and the targeting performance of medicine can be effectively improved, the blood circulation time of the medicine can be effectively prolonged, and the particles have wide application prospects.

Description

technical field [0001] The invention relates to a targeted folic acid-polyethylene glycol-lignin conjugate drug-loaded nanoparticle and a preparation method thereof, belonging to the technical field of biomedicine and nanomedicine. Background technique [0002] Nanomedicine, especially the study of biodegradable polymer nanoparticles as drug carriers, has become one of the current research hotspots. As a drug carrier, polymer nanoparticles can not only effectively increase the solubility, permeability and stability of fat-soluble drugs, but also have the characteristics of high drug loading, wide drug loading range, and long residence time in vivo. In addition, due to the relatively small particle size of nanoparticles, not only passive targeted drug delivery can be achieved, but also active targeting can be achieved by connecting ligands with specific recognition functions, thereby significantly improving the bioavailability of drugs and reducing their toxic side effects ....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/19A61K31/4745A61K47/30A61P35/00
CPCA61K9/5146A61K9/19A61K31/4745A61K47/22A61P35/00
Inventor 雷建都刘刻峰何静
Owner BEIJING FORESTRY UNIVERSITY
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