PH/reduction-sensitive nano microgel based on polyglutamic acid and cystamine

A technology of polyglutamic acid and sodium polyglutamate, which is applied in the directions of organic active ingredients, medical preparations with non-active ingredients, and medical preparations containing active ingredients, can solve problems such as a large number of organic solvents and increase the number of drugs Concentration, safety-enhancing effect

Active Publication Date: 2015-04-08
南通慧源塑胶有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The synthesis of nano-gels usually includes: inverse microemulsion crosslinking method, precipitation polymerization method, dispersion polymerization method, spray drying method and microfluidic control crosslinking method, but each method has certain defects and needs to use lots of organic solvents

Method used

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  • PH/reduction-sensitive nano microgel based on polyglutamic acid and cystamine
  • PH/reduction-sensitive nano microgel based on polyglutamic acid and cystamine
  • PH/reduction-sensitive nano microgel based on polyglutamic acid and cystamine

Examples

Experimental program
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Effect test

Embodiment 1

[0024] For the purification of polyglutamic acid, 10 g of polyglutamic acid with a weight average molecular weight of 320,000 was weighed and dissolved in 1000 mL of 0.5M NaOH solution, and stirred evenly. Slowly drop the polyglutamic acid solution dissolved in sodium hydroxide into the 1.0M HCl solution under magnetic stirring, continue to stir for 2 hours after the dropwise addition, filter out the precipitate, wash with ultrapure water, repeat the filtration and washing of the precipitate until the filtrate It is neutral, and finally the precipitate is dried in a vacuum drying oven to constant weight, and the obtained polyglutamic acid is ground into powder and placed in a desiccator for use.

Embodiment 2

[0026] Preparation of pH- and reduction-sensitive nanogels. The purified polyglutamic acid is dissolved in 0.83wt% sodium carbonate solution, and the preparation weight concentration is 0.01wt% to 0.25wt% sodium polyglutamate aqueous solution, according to polyglutamate sodium and cystamine hydrochloride The molar ratio of carboxyl group to amino group is 3:2 to 1:4. Add cystamine hydrochloride to the solution, stir at room temperature for 24 hours, put the solution into a dialysis bag with a molecular weight cut-off of 3500, and dialyze in deionized water for 72 hours to remove inorganic ions. When the solution gradually turned blue, the Tyndall phenomenon appeared in the test, and the nanometer was used to test it, and it was judged that a model of nano-microgel was formed;

[0027] The solution in the dialysis bag is transferred to the reaction bottle, and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC HCl) and N-hydroxysuccinimide (NHS), stirred and reac...

Embodiment 3

[0029] Preparation of drug-loaded nano-microgel: dissolve the dry-state nano-microgel in distilled water to form a solution with a concentration of 0.05 to 0.2w%, adjust the pH value of the solution to 7.4 with 0.5M sodium bicarbonate, and Add doxorubicin hydrochloride to 0.8 times the weight of the nano-microgel, stir magnetically for 24 hours, transfer the solution to a dialysis bag (molecular weight cut-off of 3500) and dialyze in distilled water, change fresh distilled water every four hours, and monitor the concentration of the dialysate with a conductivity meter. Sodium chloride salt concentration, until the sodium chloride salt concentration in the dialysate is less than 0.05w%.

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PUM

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Abstract

The invention provides a preparation method of pH and reduction sensitive nano microgel based on polyglutamic acid and cystamine and application of the pH and reduction sensitive nano microgel based on polyglutamic acid and cystamine in the anti-tumor aspect. The nano microgel with a particle size of 212nm is synthesized by preparing a microgel model from raw materials including rolyglutamic acid and cystamine under electrostatic interaction, and adding a catalyst to carry out crosslinking amidation reaction. Because carboxylate anions in polyglutamic acid are combined with amino cations in doxorubicin to load medicines, a high medicine lading ratio of 17.8% can be achieved. The disulfide bond in cystamine which serves as a crosslinking agent ensures that nano particles are sensitive to reduction, and the disulfide bond can break in a cancer cell containing high-concentration reduced glutathione, and thus the nano microgel is targeted at tumors and has a controlled release function. The nano microgel is directly prepared in an aqueous solution without adopting any organic solvent, and thus the safety of the medicine carrier can be guaranteed.

Description

technical field [0001] The invention relates to the preparation of a pH- and reduction-sensitive nano-microgel based on polyglutamic acid and cystamine, which belongs to the field of biomaterial preparation and drug release. Background technique [0002] Cancer is considered to be the main cause of death after cardiovascular and cerebrovascular diseases. At present, the methods for treating cancer mainly include surgical extirpation, radiotherapy and chemotherapy. But these methods all have many defects at present. For example, many anticancer drugs have the disadvantages of insoluble in water and poor stability, and not only have a killing effect on cancer cells, but also have relatively large toxic and side effects on normal cells. And after the drug enters the blood circulation system, it is usually quickly taken up by the macrophage system (MPS), reaches the target sites such as the liver, spleen, lung, bone marrow, lymph, etc. where the reticuloendothelial system (RES...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K47/34A61K9/06A61P35/00C08J3/24A61K31/704
Inventor 倪才华吴鲁艳
Owner 南通慧源塑胶有限公司
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