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Chitosan-based multi-environment-responsive type polymeric prodrug micelle and preparation method thereof

A technology of chitosan and polymer, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of low solubility of gambogic acid, limited clinical application, easy leakage of drugs, etc. problem, to achieve the effect of inhibiting growth and reproduction, improving therapeutic effect and improving solubility

Active Publication Date: 2020-07-17
XUZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the process of drug delivery, gambogic acid has a wide range of drug distribution, which is easy to cause serious side effects, including allergy, nephrotoxicity, hepatotoxicity, cardiotoxicity and neurotoxicity, etc.
In addition, the solubility of gambogic acid is extremely low (less than 0.5 μg / mL), which limits its clinical application
[0003] In order to reduce toxic side effects and improve drug efficacy, designing a nano-drug delivery system that can load anti-tumor drugs to the tumor site and release them effectively is an important goal of anti-tumor drug research. Researchers have developed a series of gambogic acid drug-loading systems However, although these drug delivery systems can improve the antitumor activity and bioavailability of gambogic acid to varying degrees, the nano drug delivery system loaded in the form of physical encapsulation has low drug loading, and storage and administration enter the systemic circulation. Disadvantages such as easy leakage of traditional Chinese medicine

Method used

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  • Chitosan-based multi-environment-responsive type polymeric prodrug micelle and preparation method thereof
  • Chitosan-based multi-environment-responsive type polymeric prodrug micelle and preparation method thereof
  • Chitosan-based multi-environment-responsive type polymeric prodrug micelle and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] (1) Preparation of folic acid-chitosan-poly(N-isopropylacrylamide) polymer: Folic acid-chitosan conjugate and amino-terminated poly(N-isopropylacrylamide) 1:4 Add the mixture of the weight ratio to 0.3% (v / v) acetic acid solution, add 1% (v / v) polysorbate 80, stir at room temperature for 1h, slowly drop glutaraldehyde solution into the reaction system, wherein folic acid -The mass ratio of chitosan conjugate, amino-terminated poly(N-isopropylacrylamide), and glutaraldehyde is 2:8:1. The reaction was continued for 1 h, and folic acid-chitosan-poly(N-isopropylacrylamide) polymer was obtained after freeze-drying.

[0039] (2) Preparation of gambogic acid and folic acid-chitosan-poly(N-isopropylacrylamide) graft polymer: gambogic acid, 1,3-dicyclohexylcarbodiimide and 4-dimethyl Aminopyridine was added to 10 mL of N,N-dimethylformamide to dissolve completely, and stirred at room temperature for 1 h in the dark. Dissolve the folic acid-chitosan-poly(N-isopropylacrylamide) ...

Embodiment 2

[0051] (1) Preparation of folic acid-chitosan-poly(N-isopropylacrylamide) polymer: the mixture of folic acid-chitosan conjugate and amino-terminated poly(N-isopropylacrylamide) Add 1:4 weight ratio to 0.3% (v / v) acetic acid solution, add 1% (v / v) poloxamer 188, stir at room temperature for 1 hour, then slowly drop glutaraldehyde solution into the reaction system, The mass ratio of folic acid-chitosan conjugate, amino-terminated poly(N-isopropylacrylamide), and glutaraldehyde is 2:8:1. Stirring is continued, and the folic acid-chitosan-poly(N-isopropylacrylamide) polymer is obtained after freeze-drying.

[0052] (2) Graft polymer of gambogic acid and folic acid-chitosan-poly(N-isopropylacrylamide): gambogic acid, 1,3-dicyclohexylcarbodiimide and 4-dimethylamino Pyridine was added to 10 mL of N,N-dimethylformamide to dissolve completely, and stirred at room temperature for 1 h in the dark. Dissolve the folic acid-chitosan-poly(N-isopropylacrylamide) polymer prepared in step (1...

Embodiment 3

[0055] (1) Preparation of folic acid-chitosan-poly(N-isopropylacrylamide) polymer: the mixture of folic acid-chitosan conjugate and amino-terminated poly(N-isopropylacrylamide) Add 1:4 weight ratio to 0.3% (v / v) acetic acid solution, add 1% (v / v) sodium dodecyl sulfate, stir at room temperature for 1 hour, then slowly drop glutaraldehyde solution into the reaction system , wherein the mass ratio of folic acid-chitosan conjugate, amino-terminated poly(N-isopropylacrylamide), and glutaraldehyde is 2:8:2. Stirring is continued, and the folic acid-chitosan-poly(N-isopropylacrylamide) polymer is obtained after freeze-drying.

[0056] (2) Graft polymer of gambogic acid and folic acid-chitosan-poly(N-isopropylacrylamide): gambogic acid, 1,3-dicyclohexylcarbodiimide and 4-dimethylamino Pyridine was added to 10 mL of N,N-dimethylformamide to dissolve completely, and stirred at room temperature for 1 h in the dark. Dissolve the folic acid-chitosan-poly(N-isopropylacrylamide) polymer p...

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Abstract

The invention discloses a chitosan-based multi-environment-responsive type polymeric prodrug micelle and a preparation method thereof. The preparation method of the chitosan-based multi-environment-responsive type polymeric prodrug micelle comprises the steps that, a folic acid-chitosan conjugate and amino-terminated poly(N-isopropylacrylamide) are used to prepare folic acid-chitosan-poly(N-isopropylacrylamide); a grafted polymer of gambogic acid and the folic acid-chitosan-poly(N-isopropylacrylamide) is prepared; and the grafted polymer is dissolved in dimethyl sulfoxide and slowly dripped into water, and the solution is subjected to dialysis and freeze-drying to obtain the micelle. Chitosan is the main component, respectively links with folic acid and the poly(N-isopropylacrylamide) which is a thermosensitive polymer material via chemical bonding, and links with the gambogic acid which is an antitumor medicine via an ester bond. A formed polymeric prodrug is multi-environment-responsive to pH, temperature and esterase.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and polymer materials, and in particular relates to a chitosan-based environment multiple responsive polymer prodrug micelle and a preparation method thereof. Background technique [0002] Gambogic acid (molecular weight 628.75) is an active ingredient extracted from the dry resin secreted from the cracks of the Latin garcinia tree. Studies have shown that gambogic acid has inhibitory effects on various tumors such as lung cancer, brain cancer, prostate cancer, pancreatic cancer, liver cancer, and leukemia. It involves a wide range of anti-tumor mechanisms, including promoting cell cycle arrest, down-regulating telomerase activity, and inducing Apoptosis, inhibition of cell proliferation, prevention of tumor cell metastasis, inhibition of channel protein expression, and anti-angiogenesis can simultaneously exert anti-tumor effects through different mechanisms, and have great ap...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/107A61K47/54A61K47/61A61K47/58A61K31/352A61P35/00A61P35/02C08G81/02
CPCA61K9/1075A61K9/19A61K31/352A61K47/545A61K47/58A61K47/61A61P35/00A61P35/02C08G81/02
Inventor 杜倩吕方南黄洁平红蕊赵子明
Owner XUZHOU MEDICAL UNIV
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