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Integrin receptor-targeted taxol nanocomposite and preparation method thereof

A technology of integrin receptors and nanocomposites, applied in the field of biomedicine, can solve problems such as organ toxicity and side effects, reduce drug therapeutic index, etc., and achieve the effect of improving therapeutic index

Inactive Publication Date: 2012-12-26
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, studies have found that after the nanoparticles enter the circulatory system, they are mainly taken up by the mononuclear phagocyte system (MPS), causing the drug to accumulate in the liver, spleen and lungs, which not only reduces the therapeutic index of the drug, but also causes damage to these organs. severe side effects

Method used

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  • Integrin receptor-targeted taxol nanocomposite and preparation method thereof
  • Integrin receptor-targeted taxol nanocomposite and preparation method thereof
  • Integrin receptor-targeted taxol nanocomposite and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Amphiphilic block copolymer HOOC-PEG-PTMC with an active group carboxyl group and a preparation method thereof, comprising the steps of:

[0035] 0.95g of HOOC-PEG (molecular weight is 3500) and 2.00g of dimethylene carbonate (TMC) were placed in a dry flask, and the toluene solution of stannous octoate was added as a catalyst. Under nitrogen protection, 140± React at 1° C. for 48 hours; the final product was dissolved in 5 ml of chloroform, and purified by precipitation with 3 times the amount of hexane. The purified product was vacuum-dried at 40°C for 24 hours to obtain the amphiphilic block copolymer HOOC-PEG-PTMC with an active group carboxyl group (stored at -20°C sealed); gel permeation chromatography (GPC) Analyze the purity of the product to 1 The molecular weight of the product was calculated from the peak area ratio of the proton in the methylene group in the H-NMR spectrum.

Embodiment 2

[0037] Amphiphilic copolymer modified with RGD peptide and preparation method thereof, comprising steps:

[0038] (1) Preparation of NHS-PEG-PTMC by activating the carboxyl group with NHS

[0039] Weigh HOOC-PEG-PTMC (0.5g, 0.053mmol), DCC (0.022g, 0.106mmol, 2×excess) and NHS (0.0122g, 0.106mmol, 2×excess) described in Example 1, dissolve In 5ml of chloroform, react at room temperature under nitrogen protection for 24 hours; after the reaction is completed, remove the solvent under reduced pressure, and precipitate with cold ether; dry the precipitate in vacuum to constant weight to obtain NHS-PEG-PTMC; 1 H-NMR spectrum is verified to product;

[0040] (2) Preparation of c(RGDyK)-PEG-PTMC with cyclic RGD peptide (c(RGDyK)) modified amphiphilic copolymer

[0041] Take the NHS-PEG-PTMC (50mg, 0.0053mmol) in the above step (1) and dissolve it in 1ml of dimethylformamide to obtain solution A; take 6.3mg (0.01mmol) of c(RGDyK) peptide and dissolve it in 0.1 M HEPES to obtain so...

Embodiment 3

[0043] Weigh 35 mg of MePEG-PTMC, 5 mg of c(RGDyK)-PEG-PTMC and 2 mg of paclitaxel, add 1 ml of dichloromethane, and ultrasonically dissolve the carrier material and drug fully. The solution was added to 5ml of 0.6% sodium cholate solution, and the ice-bath probe was sonicated with the ultrasonic power of 200 W, the ultrasonic time of 5 s, the ultrasonic interval of 5 s, and the number of ultrasonic waves 15 times. Obtain colostrum after ultrasonication, add the colostrum dropwise to 25ml of 0.3% sodium cholate solution, stir magnetically at 100r / min, after stirring for 1min, remove dichloromethane by rotary evaporation at 37°C, and obtain the entrapped Paclitaxel targeting integrin receptor nanocomplexes.

[0044] The particle size measurement results show that: the average particle size of the nanocomposite is 50.3±4.7nm.

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Abstract

The invention belongs to the technical field of biological medicines and relates to an integrin receptor-targeted taxol nanocomposite and a preparation method and application thereof. The preparation method comprises the following steps of: synthetizing a terminal carboxyl group-modified amphiphilic block copolymer HOOC-polyethylene glycol-poly trimethylene carbonate (HOOC-PEG-PTMC); connecting the amphiphilic block copolymer with a carboxyl group by an arginine-glycine-aspartic acid (RGD) polypeptide through an amido bond to obtain an RGD peptide-modified amphiphilic block copolymer; and introducing fat-soluble antitumor drug taxol into the amphiphilic block copolymer to prepare the integrin receptor-targeted taxol nanocomposite. Proved by an experimental result, the taxol nanocomposite can be used for increasing the drug concentration of the antitumor drug at a target part, reducing the accumulation of the antitumor drug at a non-target part and effectively increasing the treatment index of the drug. Shown by the result of an antitumor pharmacodynamic experiment, compared with a taxol control group, the taxol nanocomposite is more excellent in antitumor activity.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and relates to a paclitaxel nanocomposite targeting integrin receptors and a preparation method thereof. Background technique [0002] Studies have shown that tumor tissue is different from normal tissue in that it has rich blood vessels, wide space between blood vessel walls, poor structural integrity, and lack of lymphatic drainage. Therefore, drug-loaded nanoparticles can be enriched in tumor tissue through the EPR effect. However, studies have found that after the nanoparticles enter the circulatory system, they are mainly taken up by the mononuclear phagocyte system (MPS), causing the drug to accumulate in the liver, spleen and lungs, which not only reduces the therapeutic index of the drug, but also causes damage to these organs. severe toxic side effects. Therefore, building a tumor-targeted drug delivery system, reducing the damage of anti-tumor drugs to normal organs, and realizing ...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K31/337C08G64/30C08G64/42C08G65/00A61P35/00
Inventor 方晓玲姜新义沙先谊
Owner FUDAN UNIV
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