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Preparation method and application of redox-sensitive induced pH-responsive nano drug carrier

A nano-drug carrier and nano-drug technology, which can be used in drug combinations, pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve the problems of fast systemic circulation clearance rate, poor targeting, and poor controlled release effect.

Active Publication Date: 2020-10-23
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention improves the delivery efficiency of nanocarriers, realizes the controlled release of drugs in tumor cells, and can solve many problems in the prior art, such as fast systemic circulation clearance rate, poor targeting, and poor controlled release effect of nanomedicine carriers.

Method used

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  • Preparation method and application of redox-sensitive induced pH-responsive nano drug carrier
  • Preparation method and application of redox-sensitive induced pH-responsive nano drug carrier
  • Preparation method and application of redox-sensitive induced pH-responsive nano drug carrier

Examples

Experimental program
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Effect test

Embodiment 1

[0025] The synthesis of embodiment 1 monomer M1

[0026] The chemical structure of monomer M1 is shown in the figure below. The specific synthesis steps are as follows: First, add 2-aminoethyl methacrylate hydrochloride (1.65g, 10mmol) and triethylamine (2.02g, 20mmol) in a 100mL round bottom flask, add 50mL of anhydrous tetrahydrofuran to disperse Dissolve, add dropwise a solution of 2,4-dinitrobenzenesulfonyl chloride (2.66g, 10mmol) in tetrahydrofuran under ice-bath conditions, return to room temperature and react for 10h after the addition is complete. The reaction solution was distilled off the solvent under reduced pressure, and then separated by column chromatography, using ethyl acetate / petroleum ether mixture (common ratio) as the eluent, collecting the eluate containing the target compound, and after distilling off the solvent, to obtain The yield of the intermediate product 2-((2,4-dinitrophenyl)sulfonamide)ethyl methacrylate was 70%. Next, add 2-((2,4-dinitrophen...

Embodiment 2

[0030] The synthesis of embodiment 2 polymer P4

[0031]Add the reversible addition-fragmentation chain transfer polymerization (RAFT) chain transfer agent phenyl-(2-hydroxyethyl) thiocarbonate (6.1 mg, 0.1 mM) and polyethylene glycol monomethyl ether in sequence in the shlenk reaction tube Methyl methacrylate (mPEGMA) (500 mg, 1 mM) and 2-((2,4 dinitro-N-(ethyl) phenylsulfonamide) ethyl methacrylate (AMA-DNBSE) (455 mg, 1 mM ), initiator (AIBN) (1.64mg, 0.01mM) and 3mL solvent dimethylformamide (DMF), after three cycles of vacuum / argon, seal the reaction tube, and put it in an oil bath at 68-72℃ React for 24h. After the reaction, add DMF to dissolve, put it in a dialysis bag, dialyze with deionized water for 72h, and change the dialysate every 12h. After that, freeze-dry to obtain PEDF polymer. Utilize nuclear magnetic hydrogen spectrum to characterize P4 polymer , the result is attached figure 2 shown.

[0032] According to the method in embodiment 2, can obtain the poly...

Embodiment 3

[0035] The preparation method of embodiment 3 drug-loaded nanoparticles

[0036] Weigh 20 mg of PEDF polymer and 6 mg of doxorubicin, ultrasonically dissolve them with 2 mL of trifluoroethanol, and disperse them directly in 10 mL of 0.01 M phosphate buffer solution with pH=7.4 under the action of ultrasonic to obtain N4 nanoparticles with a concentration of 2mg / mL. After the solvent evaporates completely, centrifuge to remove the deposited drug, and use the laser particle size analyzer and transmission electron microscope to detect the particle size and shape of the nanoparticles. The test results are shown in the attached image 3 As shown, the nanoparticles prepared in this example have a particle size of 120 nm, a particle size distribution of 0.12, and an obvious core-shell structure. The drug-loading amount of the nano-medicine detected by an ultraviolet spectrophotometer was 2.8%.

[0037] According to the preparation method in Example 3, drug-loaded nanoparticles with...

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Abstract

The invention discloses a preparation method and an application of a redox sensitive induced pH-responsive nano drug carrier. The carrier is obtained through self-assembly of a PEDE (PEG (polyethyleneglycol)-poly-AMA-DNBSE (2-((2,4-dinitro-N-ethyl)phenyl sulfonamide)ethyl methacrylate)) amphiphilic polymer in an aqueous solution. Polymer nanoparticles have clear core-shell structures, carry hydrophobic drugs according to a similarity and intermiscibility principle and have stable properties and a passive targeted transfer function. Hydrophobic chain segments of the polymer nanoparticles contain strong electron withdrawing groups 2,4-dinitro-phenyl sulfonamide structures and can be subjected to a nucleophilic substitution reaction with sulfydryl quickly to produce secondary amine groups, and the secondary amine groups have protonation to cause disturbance to assembly stability of the nano carrier, so that the redox sensitive induced pH-responsive drug release is realized.

Description

technical field [0001] The invention relates to a preparation method and application of a redox-sensitive inducible pH-responsive nano drug carrier. Background technique [0002] In recent years, nano-drug delivery systems have great application potential in cancer treatment because of their nano-scale size, good stability, and drug-loading capacity, which can promote the accumulation of drugs in tumor sites and reduce toxic and side effects. However, most clinically used nanomedicines have not achieved breakthrough therapeutic effects. The gap between the potential of nanomedicine and clinical therapeutic effect indicates that there is a difference between carrier design and the actual physiological environment of the human body. Nano-drugs are injected intravenously to reach the tumor tissue and play a role at the molecular level. It needs to go through complex processes such as systemic circulation, tumor vascular overflow, tumor tissue enrichment and distribution, cell ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/32A61K31/704A61P35/00C08F220/38C08F220/28
CPCA61K9/5138A61K31/704C08F220/28C08F220/38C08F2438/03C08F220/286C08F220/387
Inventor 黄平升王伟伟秦怡博孔德领
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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