Novel flavone-derived polymer nano-drug and application thereof to oncotherapy

A nano-drug and tumor treatment technology, applied in drug combinations, anti-tumor drugs, medical preparations of non-active ingredients, etc., can solve the problem of diffuse distribution, low selectivity, entry into tumor tissue, and unstable aggregation of small molecule photosensitizers, etc. problem, to achieve the effect of reducing systemic side effects, high drug loading, and prolonging circulation time

Inactive Publication Date: 2018-04-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, its limitations are: most photosensitizers are very hydrophobic, and are easily removed quickly in the body, and there are agglomeration and instability, which makes it difficult to administer systemically; Consider the toxicity of the solvent; photosensitizers are easily combined with plasma proteins after entering the body, and the high binding rate makes most of them remain in the blood circulation, while only a small part may enter the tumor tissue; some researchers try to make photosensitizer mole

Method used

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  • Novel flavone-derived polymer nano-drug and application thereof to oncotherapy
  • Novel flavone-derived polymer nano-drug and application thereof to oncotherapy
  • Novel flavone-derived polymer nano-drug and application thereof to oncotherapy

Examples

Experimental program
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Effect test

Embodiment 1

[0071] Example 1: Preparation of baicalein-desulfated heparin-derived polymer

[0072] Weigh 2-bromoethylamine hydrobromide and place it in an eggplant-shaped flask, add dichloromethane as a solvent, and then add di-tert-butyl dicarbonate. The molar ratio of di-tert-butyl dicarbonate to 2-bromoethylamine hydrobromide is 1.05:1. Separately weigh N,N-dimethyl-4-pyridinamine and pipette triethylamine into a 5mL EP tube, add 2mL of dichloromethane to dissolve, and slowly drop them into the above-mentioned eggplant-shaped bottle. The molar ratio of N,N-dimethyl-4-pyridinamine to 2-bromoethylamine hydrobromide is 2:5, and the molar ratio of triethylamine to 2-bromoethylamine hydrobromide is 2:1 . After reacting at room temperature for 40 minutes, transfer to a separatory funnel and wash with 0.1mol / L dilute sulfuric acid, saturated sodium bicarbonate solution and saturated sodium chloride solution three times respectively. After washing, the organic phase was transferred to a con...

Embodiment 2

[0076] Example 2: Preparation of chrysin-low molecular weight heparin derived polymer

[0077] Weigh 3-bromopropylamine hydrobromide and place it in an eggplant-shaped flask, add dichloromethane as a solvent, and then add di-tert-butyl dicarbonate. The molar ratio of di-tert-butyl dicarbonate to 3-bromopropylamine hydrobromide is 1.1:1. Separately weigh N,N-dimethyl-4-pyridinamine and pipette triethylamine into a 5mL EP tube, add 2mL of dichloromethane to dissolve, and slowly drop them into the above-mentioned eggplant-shaped bottle. The molar ratio of N,N-dimethyl-4-pyridinamine to 3-bromopropylamine hydrobromide is 1:5, and the molar ratio of triethylamine to 3-bromopropylamine hydrobromide is 1.05:1. After reacting at room temperature for 40 minutes, transfer to a separatory funnel and wash with 0.2 mol / L dilute hydrochloric acid, saturated sodium bicarbonate solution and saturated sodium chloride solution three times respectively. After washing, the organic phase was tra...

Embodiment 3

[0081] Example 3: Preparation of quercetin-unfractionated heparin-derived polymer

[0082] Weigh 4-bromo-1-butylamine hydrobromide and place it in an eggplant-shaped flask, add dichloromethane as a solvent, and then add benzyl chloroformate. The molar ratio of benzyl chloroformate to 4-bromo-1-butylamine hydrobromide is 3:1. Separately weigh 4-pyrrolidinylpyridine, absorb triethylamine into a 5mL EP tube, add 2mL dichloromethane to dissolve, and slowly drop into the above-mentioned eggplant-shaped bottle. The molar ratio of 4-pyrrolidinylpyridine to 4-bromo-1-butylamine hydrobromide is 3:5, and the molar ratio of triethylamine to 4-bromo-1-butylamine hydrobromide is 3:1. After reacting at room temperature for 1 h, it was transferred to a separatory funnel and washed three times with 0.1 mol / L dilute sulfuric acid, saturated sodium bicarbonate solution and saturated sodium chloride solution respectively. After washing, the organic phase was transferred to a conical flask, and...

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Abstract

The invention relates to a novel flavone-derived polymer nano-drug. The novel flavone-derived polymer nano-drug is obtained in the way that hydrophobic flavone micromolecules are in covalent linkage with heparin polysaccharide macromolecules through joint arms to form an amphiphilic graft polymer, and the amphiphilic graft polymer is self-assembled in a waterborne medium to constitute a primary combination strategy of the nano-drug in oncotherapy. Hydrophobic oncotherapy drugs with different action mechanisms are loaded under such intermolecular forces as a pi-pi stacking function and a hydrophobic driving function and incorporated into a nano-system, so that the internal water solubility, the stability and the targeting property of the hydrophobic oncotherapy drugs are effectively improved to realize a secondary combination strategy of the nano-drug in oncotherapy. The nano-system loaded with the oncotherapy drugs with different mechanisms can ensure cooperation and flexible selectionaccording to clinical requirements to realize tertiary combination strategy of the nano-drug in oncotherapy. Therefore, an oncotherapy mode which attaches importance to various treatment means can berealized, and the anti-tumor effect is maximized and optimized.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to the construction of a novel flavone-derived polymer nano-medicine and its application in tumor treatment. Background technique [0002] The multidrug resistance, heterogeneity and complex relationship between tumors and the microenvironment are serious problems in the current tumor treatment. It may be difficult to achieve a good anti-tumor effect with a single treatment. At present, in clinical practice, the three main methods of tumor treatment are surgical resection, chemotherapy and radiotherapy. The above methods have played their respective advantages in tumor treatment, but at the same time, they inevitably have certain defects, such as difficult resection during surgical resection. Small lesions, easy recurrence, long radiation therapy cycle, easy damage to immune function and normal cells, and severe side effects of chemotherapy drugs. In recent years, the disco...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K31/353A61K47/36A61K45/06C08B37/00A61K47/61A61P35/00
CPCA61K31/352A61K31/353A61K45/06A61K47/36C08B37/0075
Inventor 姚静徐程于瑶
Owner CHINA PHARM UNIV
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