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RGD peptide modified boron drug loading system, preparation thereof and application of system

A drug-carrying and system technology, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and drug combinations, etc., can solve problems such as unreported research on nanocomposites, and achieve high loading and simple methods. , the effect of high release rate

Active Publication Date: 2019-10-25
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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  • RGD peptide modified boron drug loading system, preparation thereof and application of system
  • RGD peptide modified boron drug loading system, preparation thereof and application of system
  • RGD peptide modified boron drug loading system, preparation thereof and application of system

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 an RGD peptide modified boron drug loading system, preparation thereof and an application of the system. An RGD peptide modified boron composite material serves as a drug carrier for loading drugs. Experimental conditions are easily controlled, operation is simple, and an obtained drug loading compound has good biocompatibility, can be slowly released in a sustained manner, has pH (potential of hydrogen) and NIR (near-infrared light) double sensitive drug releasing properties, is high in release rate in low-pH value and near-infrared light irradiation environments andsuitable for microenvironments of tumor tissues, can be used for achieving synergistic effects of low-temperature photothermal therapy and chemotherapy and has application prospects in preparation oftumor targeted, imaging and synergistic therapy 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 Applications(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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