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Acid-sensitive polymer carrier for delivering antitumor drugs, and preparation method and application thereof

A polymer carrier and anti-tumor drug technology, applied in the field of acid-sensitive polymer carrier and preparation, can solve the problems of inability to self-assemble to form nanoparticles, lack of stable drug release, low drug loading, etc., to overcome the ineffective clinical treatment effect. Ideal, improve water solubility, reduce toxic and side effects

Active Publication Date: 2015-07-15
EAST CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the limited drug loading site (-COOH), the drug loading capacity is not high, it cannot self-assemble to form nanoparticles, and it lacks the function of stable release of drugs in tumor cells, which limits its application.

Method used

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  • Acid-sensitive polymer carrier for delivering antitumor drugs, and preparation method and application thereof
  • Acid-sensitive polymer carrier for delivering antitumor drugs, and preparation method and application thereof
  • Acid-sensitive polymer carrier for delivering antitumor drugs, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Preparation of Carboxymethylcysteine ​​Dimethyl Ester Hydrochloride

[0037]

[0038] Dissolve 10g of carboxymethylcysteine ​​(SMC) in 100ml of anhydrous methanol (analytical pure), and ice-bath to below 0°C under the protection of nitrogen, slowly add thionyl chloride solution dropwise, keep the system temperature below 0°C and stir for a while Then rise to room temperature and react for 5 hours, remove methanol by rotary evaporation at 35°C to obtain mucus, wash twice with 100 ml of ether, and vacuum-dry at room temperature for 6 hours to obtain mucus carboxymethylcysteine ​​dimethyl hydrochloride.

Embodiment 2

[0040] Preparation of polyglutamine carboxymethylcysteine ​​dimethyl ester

[0041]

[0042]Sodium polyglutamate (molecular weight 35000, 4g, 26.4mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (15.23g, 79.45mmol), 1-hydroxy Benzotriazole (4.3g, 31.82mmol), carboxymethylcysteine ​​dimethyl hydrochloride (13.77g, 56.67mmol) were dissolved in 200ml of anhydrous N,N-dimethylformamide (analytical pure) , under nitrogen protection, and stirred at 25°C for 48 hours. The solution after the reaction was slowly poured into stirred ice water to precipitate a white precipitate, which was filtered, washed three times with 200 ml of deionized water, and freeze-dried to obtain a white solid polyglutamine carboxymethyl cysteine ​​dimethyl.

Embodiment 3

[0044] Preparation of polyglutamine carboxymethylcysteine

[0045]

[0046] Polyglutaminecarboxymethylcysteine ​​dimethyl ester (1g, 3.14mmol per unit) was dissolved in 60ml of tetrahydrofuran (chemically pure), 60ml of 1mol / L lithium hydroxide aqueous solution was added, stirred for 8 hours overnight, and the tetrahydrofuran was removed by rotary evaporation. The remaining aqueous solution was adjusted to pH 3 with 2mol / L hydrochloric acid aqueous solution, poured into a dialysis bag (molecular weight cut-off 10000) and dialyzed for 24 hours, during which 4 liters of deionized water were replaced 4 times, and the resistivity of the aqueous solution outside the dialysis bag was detected. When the rate is lower than 0.1 mS / cm, collect the remaining solution in the dialysis bag, filter it with a 0.45 μm filter head, and freeze-dry to obtain white solid polyglutamine carboxymethylcysteine.

[0047] The obtained polyglutamine carboxymethylcysteine ​​is dissolved with deuterated...

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PUM

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Abstract

The invention discloses an acid-sensitive polymer carrier for delivering antitumor drugs, and a preparation method and a drug carrying application thereof. The polymer carrier is prepared through connecting sodium polyglutamate with carboxymethylcysteine through a peptide bond. The polymer carrier is used for delivering paclitaxel, doxorubicin, camptothecin and other antitumor drugs, polymer prodrugs formed through bonding the carrier with the drugs can self-assemble in water to form nanoparticles, so the water solubility and the biocompatibility of the drugs are improved, drug release is accelerated in tumor acidic environment, and the curative effects and the bioavailability of the drugs are improved.

Description

technical field [0001] The invention relates to the technical fields of polymer chemistry and nanomedicine, in particular to an acid-sensitive polymer carrier used for delivery of antitumor drugs, a preparation method and drug-carrying application. Background technique [0002] At present, chemotherapy is still one of the main means of treating tumors, but traditional small molecule tumor drugs have low clinical efficacy due to poor water solubility, lack of tumor tissue targeting, and multi-drug resistance. Linking poorly water-soluble drugs with water-soluble polymer carriers to make polymer prodrugs can significantly improve the water solubility of drugs and prolong the plasma half-life of drugs. At the same time, they can accumulate in tumor tissues through the polymer EPR effect, reducing drug toxicity Improve drug efficacy. Since the study of polymer carriers began in 1975, only a few polymer carriers have entered clinical trials, including polyethylene glycol, polygl...

Claims

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Application Information

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IPC IPC(8): C08G69/48A61K47/48A61K9/14A61K31/704A61K31/337A61K31/4745A61K31/7068A61P35/00
Inventor 王依婷肖晔南丽娟赵潇王镜俞磊朱建中董素珍闫志强
Owner EAST CHINA NORMAL UNIVERSITY
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