A kind of 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, can solve problems such as insoluble in water and difficult to use, and achieve increased intracellular throughput, small solvent consumption, and reduced Toxic effects

Active Publication Date: 2021-12-07
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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  • A kind of preparation method of targeted drug delivery nano-delivery system
  • A kind of preparation method of targeted drug delivery nano-delivery system
  • A kind of preparation method of targeted drug delivery nano-delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

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

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

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 were 68.8% and 37.52 nm.

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 were 72% and 33.56 nm.

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Abstract

The invention relates to a preparation method of a targeted drug delivery nano-delivery system. The specific steps of the method are: add NH after reacting p-methoxybenzoyl chloride and 2-bromoethylamine hydrobromic acid 2 ‑PEG‑NH‑Boc to give AEAA‑PEG‑NH‑Boc; removal of Boc with trifluoroacetic acid to give AEAA‑PEG‑NH 2 ; AEAA‑PEG‑NH 2 React with polycaprolactone-carboxylic acid to obtain polymer carrier AEAA-PEG-PCL; polymer carrier and hydrophobic drug IPI-549 self-assemble to obtain nanoparticles, which is the nano-delivery system for targeted drug delivery. The obtained polymer carrier is a targeted amphiphilic polymer, and the nanoparticles formed by self-assembly with hydrophobic drug (IPI-549) have good water solubility and small particle size, and the polymer carrier has a high encapsulation efficiency of the drug. The preparation is simple, the reaction condition is mild, and it is of great significance to the development of new preparation technology and new drug delivery system of chemotherapy 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] Nanotechnology-based drug delivery systems have become a hot spot in new chemotherapy research. It can not only increase the permeability of biofilms, improve the targeting and bioavailability of drugs, but also reduce the toxic and side effects of chemotherapeutic drugs and significantly improve the therapeutic effect. . The nano drug delivery system has the following characteristics: the 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 smoothly transported to the lesion site; the inner core can accommodate Hydrophobic drugs improve the bioavailability of poorly soluble drugs; the hydrophilic shel...

Claims

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Application Information

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Patent Type & Authority Patents(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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