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Preparation method of targeted drug delivery nano-delivery system

A technology of targeted drug delivery and delivery system, which is applied in the field of preparation of targeted drug delivery nano-delivery system, which can solve problems such as difficult to use and insoluble in water, achieve small solvent consumption, increase intracellular uptake, and synthesize simple route effect

Active Publication Date: 2020-03-06
WUHAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, IPI-549 may have the potential to treat a variety of solid tumors, but IPI-549 is extremely insoluble in water and only partially soluble in organic solvents, making it difficult to be fully utilized in the human physiological environment

Method used

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  • Preparation method of targeted drug delivery nano-delivery system
  • Preparation method of targeted drug delivery nano-delivery system
  • Preparation method of targeted drug delivery nano-delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Synthesis of a nano-delivery system for targeted drug delivery:

[0039] (1) p-Methoxybenzoyl chloride (341mg, 2mmol), 2-bromoethylamine hydrobromide (410mg, 2mmol), N,N-diisopropylethylamine (DIPEA) 180μL was dissolved in 5ml acetonitrile, React at 40°C for 12h, add NH 2 -PEG-NH-Boc(M w =2000) (400 mg, 2 mmol), stirred at room temperature for 24 hours; added 30 mL of ether to the reaction solution, centrifuged at 10,000 RCF for 10 minutes, stored at -20°C for 2 hours, and centrifuged at 8,000 RPM and -4°C for 5 minutes to form a dense For the precipitate, remove the waste ether, add new ether, vortex and centrifuge at 8000RPM and -4°C for 5 minutes to form a dense precipitate to obtain AEAA-PEG-NH-Boc with a yield of 60.2%.

[0040] (2) Re-suspend 240.8 mg of AEAA-PEG-NH-Boc in 4.5 mL of trifluoroacetic acid (TFA): dichloromethane (DCM) at a volume ratio of 1:2, and stir the solution for 2 hours. Evaporate three times, add DCM to resuspend, evaporate the solvent for...

Embodiment 2

[0047] The specific operation steps of this example are basically the same as those of Example 1, except that the mass ratio of the polymer carrier AEAA-PEG-PCL to the hydrophobic drug IPI-549 in step (4) of this example is 5:1.

[0048] The encapsulation efficiency and particle size of the nanoparticles prepared in this example are 68.8% and 37.52nm.

Embodiment 3

[0050] The specific operation steps of this example are basically the same as those of Example 1, except that the mass ratio of the polymer carrier AEAA-PEG-PCL to the hydrophobic drug IPI-549 in step (4) of this example is 10:1.

[0051] The encapsulation efficiency and particle size of the nanoparticles prepared in this example are 72% and 33.56nm.

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Abstract

The invention relates to a preparation method of a targeted drug delivery nano-delivery system, which comprises the following steps: reacting p-methoxybenzoyl chloride with 2-bromoethylamine hydrobromic acid, and adding NH2-PEG-NH-Boc to obtain AEAA-PEG-NH-Boc; removing Boc through trifluoroacetic acid to obtain AEAAA-PEG-NH2; reacting the AEAA-PEG-NH2 with polycaprolactone-carboxylic acid to obtain a polymer carrier AEAA-PEG-PCL; and self-assembling the polymer carrier and a hydrophobic drug IPI-549 to obtain nanoparticles which can be the targeted drug delivery nano-delivery system. The obtained macromolecular carrier is the amphiphilic polymer with targeting property, nanoparticles formed by self-assembly of the macromolecular carrier and the hydrophobic drug (IPI-549) are good in watersolubility and small in particle size, the encapsulation efficiency of the macromolecular carrier on the drug is high, the preparation is simple, and the reaction conditions are mild, which has important significance in developing a new preparation technology and a new drug delivery system of chemotherapeutic drugs.

Description

technical field [0001] The invention relates to the technical field of nano-medicine, in particular to a preparation method of a targeted drug delivery nano-delivery system. Background technique [0002] The nano drug delivery system based on nanotechnology has become a hot spot in the research of new chemotherapy. It can not only increase the permeability of biomembrane, improve the targeting and bioavailability of drugs, but also reduce the toxic and side effects of chemotherapy drugs, and significantly improve the therapeutic effect. . The nano-drug loading system has the following characteristics: the outer shell is hydrophilic, the overall size is small and the specific surface area is large, which can reduce the recognition and uptake of the reticuloendothelial system, so that the drug can penetrate the biological barrier and be transported to the lesion smoothly; the inner core can accommodate Hydrophobic drugs can improve the bioavailability of insoluble drugs; poly...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/52A61K47/34A61K47/18A61K31/519A61P35/00
CPCA61K9/5123A61K9/5153A61K31/519A61P35/00
Inventor 郑化姜敏张雪琼孙佳慧杨梦佳
Owner WUHAN UNIV OF TECH
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