Hypoxia-responsive chiral drug micelles targeting triple-negative breast cancer and preparation methods thereof

A technology of triple-negative breast cancer and chiral drugs, applied in drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., to achieve the effects of prolonging stability, improving anti-tumor effects, and prolonging circulation time

Active Publication Date: 2022-01-28
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few studies on drug carriers based on azo-hypoxic response, and we need to design effective azo-hypoxic-responsive nanocarriers to meet the challenge of hypoxic environment encountered in traditional tumor therapy.

Method used

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  • Hypoxia-responsive chiral drug micelles targeting triple-negative breast cancer and preparation methods thereof
  • Hypoxia-responsive chiral drug micelles targeting triple-negative breast cancer and preparation methods thereof
  • Hypoxia-responsive chiral drug micelles targeting triple-negative breast cancer and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0037] Preparation of AS1411 modified polyethylene glycol-azobenzene-dextrorotary polylactic acid block copolymer:

[0038] (1) Dissolve 50 mg (1 equivalent) of carboxypolyethylene glycol active ester (COOH-PEG-NHS, MW=1000) in 6 mL of dichloromethane, and add 6.8 mg (1.3 equivalents) of 4,4-azobis Aniline (AZO), after reacting for 24 hours at room temperature under stirring in the dark, concentrate the reaction solution obtained from the reaction, add 25mL of glacial ether for purification, let it stand overnight and then centrifuge, and dry the precipitate obtained by centrifugation to obtain carboxypolyethylene glycol azobenzene (COOH-PEG-AZO-NH 2 );

[0039] (2) Dissolve 50 mg (1.3 equivalents) of carboxy-dextrorotary polylactic acid (COOH-PDLA, MW=2000) in 5 mL of dichloromethane, and add 8 mg (2 equivalents) of dicyclohexylcarbodiimide (DCC) and 5 mg ( 2.3 equivalents) of N-hydroxysuccinimide (NHS), after stirring for 30 minutes at room temperature, add 41 mg (1 equiva...

Embodiment 1-2

[0042] Preparation of AS1411 modified polyethylene glycol-azobenzene-dextrorotary polylactic acid block copolymer:

[0043] Carboxylated polyethylene glycol active ester (COOH-PEG-NHS, MW=1000) in step (1) of Example 1-1 was replaced by carboxylated polyethylene glycol active ester (COOH-PEG-NHS, MW=2000) , and then prepare AS1411-modified polyethylene glycol-azobenzene-dextrorotatory polylactic acid block copolymer (AS1411-PEG-AZO-PDLA) according to step (2) and step (3) of Example 1-1.

Embodiment 1-3

[0045] Preparation of AS1411 modified polyethylene glycol-azobenzene-dextrorotary polylactic acid block copolymer:

[0046] Carboxylated polyethylene glycol active ester (COOH-PEG-NHS, MW=1000) in step (1) of Example 1-1 was replaced by carboxylated polyethylene glycol active ester (COOH-PEG-NHS, MW=5000) , and then prepare AS1411-modified polyethylene glycol-azobenzene-dextrorotatory polylactic acid block copolymer (AS1411-PEG-AZO-PDLA) according to step (2) and step (3) of Example 1-1.

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Abstract

The invention belongs to the technical field of nano-pharmaceuticals, and discloses a hypoxia-responsive chiral drug micelle targeting triple-negative breast cancer and a preparation method thereof. The preparation method of the present invention first introduces the azophenyl group into the molecular chain of carboxypolyethylene glycol active ester to obtain carboxypolyethylene glycol azobenzene, and then prepares carboxypolyethylene glycol by reacting it with carboxyl D-polylactic acid. Diol-azobenzene-dextrorotary polylactic acid block copolymer, and then introduce amino-modified nucleic acid aptamer AS1411 to prepare AS1411 modified polyethylene glycol-azobenzene-dextrorotary polylactic acid, a complex fat-soluble anti- After the cancer drug is dialyzed, the micelles of the present invention are obtained. The hypoxia-responsive chiral drug micelles provided by the present invention have small particle size and narrow distribution, and can effectively stay at the target site; have hypoxia responsiveness, and achieve the effect of hypoxia sustained release; can target TNBC tumors, and select Sexual release of anti-cancer drugs, significantly improving the anti-tumor effect.

Description

technical field [0001] The invention belongs to the technical field of nano-pharmaceuticals, and in particular relates to a hypoxia-responsive chiral drug micelle targeting triple-negative breast cancer and a preparation method thereof. Background technique [0002] Breast cancer is the most common malignant tumor in women all over the world, and 90% of the deaths of breast cancer patients are caused by tumor metastasis. As a subtype of breast cancer, triple-negative breast cancer (TNBC) has the worst survival rate because of its highly metastatic and invasive tumor cells. At the same time, the cancer cell population of TNBC often develops drug resistance due to its high invasiveness and self-renewal ability. This makes the free drug therapy ineffective, unable to eradicate cancer cells, and unable to stop tumor metastasis process. [0003] Nano-drug carrier is a sub-particle drug carrier delivery system belonging to the category of nano-scale microcosm. Nanomedicines sma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/34A61K47/10A61K31/704A61K31/337A61K31/4745A61P35/00
CPCA61K9/1075A61K47/34A61K47/10A61K31/704A61K31/337A61K31/4745A61P35/00
Inventor 陈忠平陆敏刘雪蒙龙朦朦翁凌燕朱俐
Owner NANTONG UNIVERSITY
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