Reduced sensitive type polymer with effect of arginine membrane penetration as well as preparation method and application of reduced sensitive type polymer

An arginine and polymer technology, applied in the field of medical materials, can solve the problems of low drug bioavailability and slow entry of drug-loaded micelles into cancer cells, so as to improve the therapeutic effect, speed up the entry into cells, and reduce toxic and side effects Effect

Active Publication Date: 2015-11-11
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above-mentioned drug-loaded micelles can accumulate in tumor tissues through the EPR effect, adding a carrier protective layer to the small drug molecules will inevitably add a layer of barriers to the diffusion of small drug molecules into cancer cells, resulting in the entry of drug-loaded micelles into cancer cells. Cancer cells are slower
However, the environment in the body is very complex, and the drug-loaded micelles accumulated in the tumor tissue are foreign substances to the body itself. systemic circulation is cleared by the body's own immune system, resulting in lower bioavailability of the drug

Method used

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  • Reduced sensitive type polymer with effect of arginine membrane penetration as well as preparation method and application of reduced sensitive type polymer
  • Reduced sensitive type polymer with effect of arginine membrane penetration as well as preparation method and application of reduced sensitive type polymer
  • Reduced sensitive type polymer with effect of arginine membrane penetration as well as preparation method and application of reduced sensitive type polymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] In this example, the structural formula of the reduction-sensitive polymer with arginine transmembrane effect is:

[0053]

[0054] Its preparation method is as follows:

[0055] (1) Preparation of cystamine bisacrylamide monomer (BCA)

[0056] Metering cystamine dihydrochloride, acryloyl chloride and sodium hydroxide according to the molar ratio of cystamine dihydrochloride, acryloyl chloride and acid scavenger sodium hydroxide is 1:. The volume ratio of 1:10 is mixed to form a mixed solution, and cystamine dihydrochloride is dissolved in deionized water to form a cystamine dihydrochloride aqueous solution with a cystamine dihydrochloride concentration of 10mol / L, and sodium hydroxide is dissolved in Form the sodium hydroxide aqueous solution that sodium hydroxide concentration is 20mol / L in deionized water;

[0057] Mix the mixture of acryloyl chloride and dichloromethane with the aqueous solution of cystamine dihydrochloride to form a reaction system, add the ab...

Embodiment 2

[0070] In this example, the structural formula of the reduction-sensitive polymer with arginine transmembrane effect is:

[0071]

[0072] Its preparation method is as follows:

[0073] (1) Preparation of cystamine bisacrylamide monomer (BCA)

[0074]Metering cystamine dihydrochloride, acryloyl chloride and sodium hydroxide according to the molar ratio of cystamine dihydrochloride, acryloyl chloride and acid scavenger sodium hydroxide is 1:2:4, and acryloyl chloride and dichloromethane according to 1 : the volume ratio of 0.1 is mixed to form a mixed solution, and cystamine dihydrochloride is dissolved in deionized water to form a cystamine dihydrochloride solution with a cystamine dihydrochloride concentration of 1moL / L, and sodium hydroxide is dissolved in deionized water Form the sodium hydroxide aqueous solution that sodium hydroxide concentration is 1moL / L in ionized water;

[0075] Mix the mixture of acryloyl chloride and dichloromethane with cystamine dihydrochlori...

Embodiment 3

[0088] In this example, the structural formula of the reduction-sensitive polymer with arginine transmembrane effect is:

[0089]

[0090] Its preparation method is as follows:

[0091] (1) Preparation of cystamine bisacrylamide monomer (BCA)

[0092] Metering cystamine dihydrochloride, acryloyl chloride and potassium hydroxide according to the molar ratio of cystamine dihydrochloride, acryloyl chloride and acid scavenger potassium hydroxide is 1:10:8, and acryloyl chloride and dichloromethane according to 1 The volume ratio of 10 is mixed to form mixed liquor, and cystamine dihydrochloride is dissolved in deionized water to form cystamine dihydrochloride concentration and is the cystamine dihydrochloride aqueous solution of 100moL / L, potassium hydroxide is dissolved in deionized water Form potassium hydroxide concentration in ionized water and be the potassium hydroxide aqueous solution of 25moL / L;

[0093] Mix the mixture of acryloyl chloride and dichloromethane with cy...

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Abstract

The invention provides a reduced sensitive type polymer with the effect of arginine membrane penetration as well as a preparation method of the reduced sensitive type polymer. The polymer can self-assemble in an aqueous medium to form micelle of a shell-core structure; the polymer contains a poly-L-arginine structure, so that the speed that the polymer penetrates through a cell membrane to enter cancer cells is increased; meanwhile, the polymer contains a disulfide bond, so that the polymer can be degraded by relatively high reduction potential energy in cancer cells. The invention further provides application of the reduced sensitive type polymer with the effect of arginine membrane penetration as a drug carrier. After being gathered at tumor tissue through the enhanced permeability and retention effect, the carrier can quickly enter the cancer cells, so that bioavailability and the treatment effect of the drug can be improved.

Description

technical field [0001] The invention belongs to the field of medical materials, and in particular relates to a reduction-sensitive polymer with arginine transmembrane function and a preparation method thereof, and the application of the reduction-sensitive polymer with arginine transmembrane function as a drug carrier. Background technique [0002] Cancer has become one of the greatest threats to human health. Chemotherapy is an important means of treating cancer at present, but traditional anticancer drug preparations have poor selectivity in the body. Most anticancer drugs kill cancer cells and also damage normal tissues. Produce certain toxicity and cause the death of normal cells. In recent years, the research and development of anti-tumor targeted drug delivery system for the purpose of drug safety and high-efficiency treatment, especially the anti-tumor targeted drug delivery system of polymer micelles, has become one of the research hotspots of pharmaceutical preparat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00C08G73/02A61K47/34A61K9/107A61K47/48A61K45/00A61K38/00A61K48/00A61P35/00
Inventor 孙勇樊渝江崔亚妮随俊慧张兴栋
Owner SICHUAN UNIV
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