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PH-responsive block copolymer, nano particle, preparation method and drug

A block copolymer and nanoparticle technology, which can be used in drug combinations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Improve stability, overcome the effect of low solubility

Active Publication Date: 2020-06-05
HEBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, nano-drug carriers still have some defects, such as premature release of drugs will produce toxic and side effects, and non-targeted drug release will reduce the therapeutic effect of the lesion. Precise drug release is an effective way to improve the therapeutic effect of nano-carriers

Method used

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  • PH-responsive block copolymer, nano particle, preparation method and drug
  • PH-responsive block copolymer, nano particle, preparation method and drug
  • PH-responsive block copolymer, nano particle, preparation method and drug

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preparation example Construction

[0049]According to another aspect of the present invention, the present invention also provides a preparation method of the above block copolymer. The invention adopts a reversible addition-fragmentation chain transfer polymerization method (RAFT polymerization method), including: synthesizing RAFT reagent PEO-CTA containing a chain transfer agent; then reacting PEO-CTA with DMAEMA, MAEBA initiator and solvent after mixing. An embodiment of concrete reaction process is as follows:

[0050]

[0051] In some preferred embodiments, PEO-CTA, DMAEMA, MAEBA and the solvent are mixed and then degassed, then placed in a sealed container at 65-75°C for 5.5-6.5 hours and then rapidly cooled to room temperature; the reaction temperature can be, for example, but Not limited to 65°C, 66°C, 67°C, 68°C, 69°C, 70°C, 71°C, 72°C, 73°C, 74°C or 75°C; the reaction time can be but not limited to 5.5h, 5.6h, 5.7 h, 5.8h, 5.9h, 6.0h, 6.1h, 6.2h, 6.3h, 6.4h, or 6.5h. In some preferred embodiment...

Embodiment 1

[0074] Preparation of pH responsive block copolymer PEO-b-P (DMAEMA-co-MAEBA), comprises the steps:

[0075] (a) Monohydroxypolyethylene oxide m-PEO 44 (20g, 0.01mol), carboxyl-containing chain transfer agent CTA (7.28g, 0.02mol), dicyclohexylcarbodiimide DCC (2.06g, 0.01mol), 4-dimethylaminopyridine DMAP (0.0127g, 0.001mol) was dissolved in 100mL DCM, reacted at room temperature for 24h, and precipitated in ether to obtain a yellow powder.

[0076] (b) Add PEO-CTA (250mg, 0.05mmol), DMAEMA (471mg, 3mmol), MAEBA (234mg, 1mmol), AIBN (1.64mg, 0.01mmol), THF (2ml) into a 5mL polymerization tube, respectively.

[0077] (c) Degas the mixture of step (b) through three freeze-dry-pump-thaw cycles.

[0078] (d) Flame-seal the polymerization tube under vacuum, soak the sealed tube in an oil bath at 70°C, react for 6 hours, and then rapidly cool the polymerization tube to room temperature.

[0079] (e) The reaction product was separated by n-hexane precipitation, filtered and then v...

Embodiment 2

[0082] Using the pH-responsive block copolymer prepared in Example 1 to prepare pH-responsive nanoparticles embedding CaCCinh-A01 includes the following steps:

[0083] (A) 10 mg of the block copolymer PEO-b-P (DMAEMA-co-MAEBA) and 10 mg of the drug to be embedded CaCCinh-A01 were dissolved in 1 mL of THF.

[0084] (B) Under vigorous stirring, add deionized water at a rate of 9mL / h through a syringe pump, add a total of 9mL of deionized water, after the addition is complete, stir and disperse for 5h.

[0085] (C) Dialyze against deionized water (molecular weight cut-off (MWCO): 35kda), remove THF for 48 hours, and replace the dialysis medium every 12 hours, and the prepared pH-responsive nanoparticles loaded with drugs are as follows: figure 2 shown.

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Abstract

The invention provides a pH-responsive segmented copolymer, a nano particle, a preparation method and a drug, and relates to the technical field of drug carriers. The block copolymer with pH responsiveness is formed by polymerizing PEO (Polyethylene Oxide), MAEBA (Methyl Acetate Ethylene Benzene Acetate) and DMAEMA (Dimethyl aminoethyl Methacrylate), the pH responsive nano particle can be formed in a water solution through self-assembly, a micelle core layer is composed of hydrophobic MAEBA and a pH responsive unit DMAEMA, a micelle shell is formed by hydrophilic PEO, conformational change occurs in a low-pH environment, and the nano particles becomes pH-sensitive. When the pH-responsive block copolymer or pH-responsive nano particle are used as a carrier to carry a drug, the drug releasesthe active pharmaceutical ingredients in the drug when the pH environment is changed, so that the drug has a targeting property.

Description

technical field [0001] The invention relates to the technical field of drug carriers, in particular to a pH-responsive block copolymer and nanoparticles, a preparation method and a drug. Background technique [0002] At present, nanomaterials are widely used in biomedical fields such as drug delivery, magnetic resonance imaging, bioseparation, fluorescence imaging, and photothermal therapy. Due to the unique nano-effects of nanocarriers, they become targeted delivery tools for drugs or genes. Nanocarriers currently mainly include liposomes, nanomicelles, polymers, dendrites, magnetic nanoparticles, and carbon nanotubes. However, at present, nano-drug carriers still have some defects. For example, premature release of drugs will cause toxic and side effects, and non-targeted drug release will reduce the therapeutic effect of the lesion. Precise drug release is an effective way to improve the therapeutic effect of nano-carriers. Therefore, an improved nanocarrier capable of ...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F220/34C08F220/30A61K9/107A61K47/34A61K31/381A61P35/00
CPCC08F293/005C08F220/34C08F220/30A61K9/1075A61K47/34A61K31/381A61P35/00C08F2438/03
Inventor 安海龙陈娅斐郭帅邱亮展永
Owner HEBEI UNIV OF TECH
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