A targeted nanoparticle for inhibiting breast cancer and its preparation and application

A nanoparticle, breast cancer technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the drug resistance of tumor cell heterogeneity chemotherapy drugs and affect the treatment effect of patients Prognosis and other issues, to achieve the effect of reversing the drug resistance mechanism and enhancing the therapeutic effect

Active Publication Date: 2020-12-15
SOUTH CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the heterogeneity of tumor cells and the resistance to chemotherapeutic drugs, the treatment effect and patient prognosis are seriously affected.

Method used

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  • A targeted nanoparticle for inhibiting breast cancer and its preparation and application
  • A targeted nanoparticle for inhibiting breast cancer and its preparation and application
  • A targeted nanoparticle for inhibiting breast cancer and its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1 Preparation of a targeted nanoparticle for inhibiting breast cancer

[0068] 1. Preparation method

[0069] (1) Carboxylation of doxorubicin:

[0070] Measure 4 ml of dimethylformamide (DMF), add to a beaker, weigh 10 mg of dicyclohexylcarbodiimide (DCC), 1 mg of 4-dimethylaminopyridine (DMAP), 5 mg of Oxalic acid, mixed and stirred for 30 min, added 500 μl 1mg / ml doxorubicin (DOX), stirred at room temperature with a magnetic stirrer for 3 h, collected the reaction solution into a centrifuge tube, centrifuged at 5000 rpm for 10 min, collected the supernatant, added 5 ~7 times the volume of water, shake well, add 2 volumes of ethyl acetate, extract 3 times, collect the ethyl acetate layer, use a dialysis bag for 12 h dialysis, and freeze-dry to obtain orange crystals, which are carboxylated albino Mycin.

[0071] (2) Esterification reaction of proanthocyanidins and lecithin

[0072] Measure 4 ml of DMF, add it into a beaker, weigh 10 mg of DCC, 1 mg of DMAP...

Embodiment 2

[0081] Example 2 Preparation of a targeted nanoparticle for inhibiting breast cancer

[0082] 1. Preparation method

[0083] (1) Carboxylation of doxorubicin:

[0084] Measure 3 ml of dimethylformamide (DMF), add to a beaker, weigh 9 mg of dicyclohexylcarbodiimide (DCC), 0.9 mg of 4-dimethylaminopyridine (DMAP), 4.5 mg of Oxalic acid, mixed and stirred for 30 min, added 450 μl 1mg / ml doxorubicin (DOX), stirred at room temperature with a magnetic stirrer for 3 h, collected the reaction liquid into a centrifuge tube, centrifuged at 5000 rpm for 10 min, collected the supernatant, added 5- 7 times the volume of water, shake well, add 2 volumes of ethyl acetate, extract 3 times, collect the ethyl acetate layer, use a dialysis bag for 12 hours of dialysis, and freeze-dry to obtain orange crystals, which are carboxylated doxorubicin white.

[0085] (2) Esterification reaction of proanthocyanidins and lecithin

[0086] Measure 3 ml of DMF, add it into a beaker, weigh 9 mg of DCC, ...

Embodiment 3

[0095] Example 3 Preparation of a targeted nanoparticle for inhibiting breast cancer

[0096] 1. Preparation method

[0097] (1) Carboxylation of doxorubicin:

[0098] Measure 5 ml of dimethylformamide (DMF), add to a beaker, weigh 11 mg of dicyclohexylcarbodiimide (DCC), 1.1 mg of 4-dimethylaminopyridine (DMAP), 5.5 mg of Oxalic acid, mixed and stirred for 30 min, added 550 μl 1mg / ml doxorubicin (DOX), stirred at room temperature with a magnetic stirrer for 3 h, collected the reaction liquid into a centrifuge tube, centrifuged at 5000 rpm for 10 min, collected the supernatant, added 5- 7 times the volume of water, shake well, add 2 volumes of ethyl acetate, extract 3 times, collect the ethyl acetate layer, use a dialysis bag for 12 hours of dialysis, and freeze-dry to obtain orange crystals, which are carboxylated doxorubicin white.

[0099] (2) Esterification reaction of proanthocyanidins and lecithin

[0100] Measure 5 ml of DMF, add it into a beaker, weigh 11 mg of DCC...

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Abstract

The invention discloses a targeted nano-particle for inhibiting breast cancer, and a preparation method and an application thereof. The nano-particle is obtained through modifying procyanidin, catechin, doxorubicin and lecithin, performing dehydration condensation, and grafting the obtained substance with a breast cancer-specific ligand. The preparation process of the nano-particle for targeting breast cancer cells in the invention is simple, and the product has a good stability, a good dispersibility and a good homogeneity, realizes the organic combination of a natural drug, a synthetic drugand biological targeting, has a good cell penetrability, has extremely strong specific targeting capability, and forms a novel treatment system for inhibiting the growth of breast cancer cells. The nano-particle can reduce adverse effects of drugs while improving the targeted treatment of tumors. Above characteristics of the nano-particle provide a new development direction for clinically targetedtumor therapy and further promote the development of a nano-carrier drug delivery system.

Description

technical field [0001] The invention relates to the technical field of biomedical materials, and more specifically, relates to a targeted nanoparticle for inhibiting breast cancer. Background technique [0002] Nano-healthy material technology is an emerging technology. Nano-materials synthesized by nano-healthy material technology have high intestinal absorption efficiency, high bioavailability, sustainable and targeted transport capabilities, effectiveness, good in vivo stability, and solubility. The excellent characteristics of good and other aspects have been widely used in the diagnosis and treatment of diseases, and nanomaterials as drug carriers have become a hot spot in the field of nanomedicine research. After the small molecule drug is loaded by the nanocarrier, it can accumulate at the lesion site, exert a sustained release effect, enhance the killing effect on the target cells, and reduce the damage of the small molecule drug to the surrounding healthy tissue. I...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/68A61K47/54A61K31/704A61K31/352A61K31/353A61P35/00
CPCA61K31/352A61K31/353A61K31/704A61K2300/00
Inventor 关燕清杜世伟胡卓妍
Owner SOUTH CHINA NORMAL UNIVERSITY
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