A boron drug-loaded system modified by rgd peptide and its preparation and application

A drug loading and system technology, applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, drug combinations, etc., can solve the problems of nanocomposites that have not been reported yet, and achieve high loading capacity and excellent reaction conditions. Gentle, easy-to-apply results

Active Publication Date: 2021-11-23
河北英治医疗器械科研有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To the best of our knowledge, the study of constructing B NSs-based nanocomposites using a synergistic therapeutic strategy of low-temperature photothermal therapy and chemotherapy has not been reported yet.

Method used

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  • A boron drug-loaded system modified by rgd peptide and its preparation and application
  • A boron drug-loaded system modified by rgd peptide and its preparation and application
  • A boron drug-loaded system modified by rgd peptide and its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] (1) The preparation method of boron nanosheets is: disperse 0.5g boron powder (purchased from Shanghai Aladdin Chemical Reagent Co., Ltd.) in 100mL mixed NMP (N-methyl-2-pyrrolidone) and ethanol (1:1, In v / v), the ice-bath probe was sonicated for 5 h and then centrifuged at 3,000 rpm for 10 min to discard large pieces of B. The supernatant was centrifuged at 12,000 rpm for 20 min, washed with ethanol three times, and then the ethanol was removed by vacuum rotary evaporation. The collected B pieces were placed in a crucible and heated at 650 °C for 2 h. After the reaction, the product was collected and subjected to probe sonication in water. Finally, the resulting mixture was centrifuged at 12,000 rpm for 30 min to collect the precipitate.

[0045] (2) Add 10mg of H 2 N-PEG-NH 2 (MW: 2000Da, purchased from Shanghai Yayi Biotechnology Co., Ltd.) was dispersed in 10 mL of B NSs (B concentration: 200 μg / mL) aqueous solution. After sonication for 30 min and magnetic sti...

Embodiment 2

[0054] (1) The preparation method of boron nanosheets is: disperse 0.5g of boron powder in 100mL mixed NMP (N-methyl-2-pyrrolidone) and ethanol (1:1, v / v), and ultrasonically After 5 h of treatment, centrifuge at 3,000 rpm for 10 min to discard bulk B. The supernatant was centrifuged at 12,000 rpm for 20 min, washed with ethanol three times, and then the ethanol was removed by vacuum rotary evaporation. The collected B pieces were placed in a crucible and heated at 650 °C for 2 h. After the reaction, the product was collected and subjected to probe sonication in water. Finally, the resulting mixture was centrifuged at 12,000 rpm for 30 min to collect the precipitate.

[0055] (2) Add 10mg of H 2 N-PEG-NH 2 Disperse in 10 mL of B NSs / H 2 O (B concentration is 200μg / mL) solution. After sonication for 30 min and magnetic stirring for 12 h, the resulting mixture was centrifuged at 2500 rpm (4 °C) for 30 min to remove unloaded H 2 N-PEG-NH 2 molecules, and washed 3 times in...

Embodiment 3

[0062] Seed MDA-MB-231 cells in a 96-well plate, the number of cells per well is about 10,000, add 200 μL of DMEM full medium to each well, and store at 37°C and 5% CO 2Cultured in a constant temperature incubator for 24 hours. Then remove the old medium, wash with PBS buffer and add 20 μL of different concentrations of B-PEG-cRGD, free DOX, DOX-17AAG@B-PEG, DOX@B-PEG-cRGD, DOX-17AAG@B to each well -PEG-cRGD solution, supplemented with 180 μL of fresh medium, and continued to culture in a constant temperature incubator for 24 hours. Among them, the B-PEG-cRGD+NIR, DOX@B-PEG-cRGD+NIR, DOX-17AAG@B-PEG-cRGD+NIR groups had a power of 0.5W / cm 2 After irradiating with 808nm laser for 30min, continue to culture in constant temperature incubator (total 24h). Add 20 μL of 5 mg / mL MTT solution, incubate in the incubator for 4 hours, remove the culture medium in the wells, and add 200 μL DMSO, place on a shaker and shake at low speed for 15-20 minutes in the dark, and use an enzyme-lin...

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Abstract

The invention relates to a boron drug-carrying system modified by RGD peptide and its preparation and application. The boron composite material modified by RGD peptide is used as a drug carrier to load drugs. The experimental conditions of the present invention are easy to control and simple to operate; the obtained drug-loaded complex has good biocompatibility, can be long-acting and sustained release, and has dual sensitive drug release properties of pH and near-infrared light (NIR). Value and high release rate under near-infrared light irradiation environment, suitable for the microenvironment of tumor tissue, can be used for the synergistic effect of combined low-temperature photothermal therapy and chemotherapy, and has application prospects in the preparation of tumor targeting, imaging and synergistic therapeutic drugs.

Description

technical field [0001] The invention belongs to the field of drug-carrying system and its preparation and application, in particular to a boron drug-carrying system modified by RGD peptide and its preparation and application. Background technique [0002] Malignant tumors seriously threaten human health and life, and tumor treatment has become a major challenge in the current medical research field. At present, the treatment methods for tumors are mainly surgical resection, radiotherapy, and chemical drug therapy, and at the same time, gene therapy and biological therapy are used as adjuvant therapy. Doxorubicin is a broad-spectrum and highly effective anti-tumor drug, which mainly inhibits the synthesis of nucleic acids by intercalating DNA, so as to achieve the killing effect on tumor cells. However, most antineoplastic drugs exhibit high dose-induced cytotoxicity and side effects caused by insufficient specificity and targeting. Among them, the most unfavorable point is...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/64A61K47/60A61K41/00B82Y5/00B82Y20/00B82Y30/00A61P35/00B82Y40/00A61K31/395A61K31/704
CPCA61K31/395A61K31/704A61K41/0042A61K41/0052A61K47/60A61K47/64A61K47/6923A61P35/00B82Y5/00B82Y20/00B82Y30/00B82Y40/00A61K2300/00
Inventor 朱利民付梓吴建荣
Owner 河北英治医疗器械科研有限公司
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