Specific targeted breast cancer cell mesoporous silicon nanometer drug loading system and preparation method thereof

A breast cancer cell and nano-drug loading technology, which is applied in the research and development and preparation of cancer cell-targeted drugs, can solve problems such as limiting the effect of clinical treatment, and achieve the effects of efficient chemotherapy drug delivery, good stability, and accelerated drug release

Inactive Publication Date: 2018-10-19
马鞍山市人民医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, gastrointestinal reactions, cardiotoxicity, and other drug side effects due to non-specificity due to cytotoxicity limit the efficacy of clinical treatment

Method used

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  • Specific targeted breast cancer cell mesoporous silicon nanometer drug loading system and preparation method thereof
  • Specific targeted breast cancer cell mesoporous silicon nanometer drug loading system and preparation method thereof
  • Specific targeted breast cancer cell mesoporous silicon nanometer drug loading system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Preparation and characterization of specific targeted drug-loaded MSN system

[0026] Weigh 0.3198g CTAB + 2.815ml EtOAc + 545.0ml H2O + 9.695ml NH4OH, stir to fully dissolve CTAB, add (0.72mlTEOS + 0.88ml APTES) mixture (mixed by pipetting more than 20 times), and react at 22°C for 24h; Centrifuge at 13000rpm for 30min, wash with ultrasonic ethanol twice, and react the obtained sample + (240ml ethanol + 480ul concentrated HCL) at 60°C for 3h. Using the method of chemical synthesis, different experimental conditions were changed to synthesize mesoporous silica nanoparticles with different sizes and particle diameters. The nanoparticles were examined by scanning electron microscopy. The results of electron microscopy showed that the mesoporous silica particles were uniform and the pore size was the same. Evenly distributed (such as figure 1 shown).

[0027] According to the principle that the surface of mesoporous silica is rich in amino groups, YSA and D4 s...

Embodiment 2

[0029] Example 2: In vitro slow-release experiment of specifically targeting highly expressed EGFR drug-loaded MSN system

[0030] To confirm the loading efficiency of doxorubicin by the same weight of mesoporous silica (MSN) nanomaterials under different pH conditions. The specific operation is briefly described as follows: Dissolve 2 mg of mesoporous silica material and 0.5 mg of doxorubicin in 1 mL of phosphate buffered saline (PBS) with different pH values, shake and mix overnight at room temperature, and centrifuge at 12,000 rpm for 30 minutes , and the supernatant was taken to measure the loading efficiency of the same concentration of doxorubicin in the mesoporous silica in solutions with different pH values ​​by spectrophotometer. In a neutral alkaline (pH7.4) environment similar to normal human body fluids, the drug loading capacity of mesoporous silica is the largest, and the drug content in the centrifuged supernatant is the lowest. When the solution is acidic (pH5...

Embodiment 3

[0031] Example 3: The in vitro uptake experiment of breast cancer cell MCF7 to the specific targeting drug-loaded MSN system

[0032] Doxorubincin (DOX), also known as doxorubicin, is the most commonly used tumor chemotherapy drug. This chemotherapy drug can be used for acute leukemia, malignant lymphoma, breast cancer, lung cancer, ovarian cancer, bone and soft tissue sarcoma, nephritis Cell tumor, bladder cancer, thyroid cancer, prostate cancer, head and neck squamous cell carcinoma, testicular cancer, gastric cancer, liver cancer, etc. The chemotherapeutic drug has good water solubility, and the most important thing is that the drug emits red fluorescence under ultraviolet irradiation, and the fluorescence intensity can be observed with a fluorescence microscope to judge the nanoparticles entering the cells.

[0033]When breast cancer MCF7 cells were subcultured for 24 hours and the fusion rate between cells reached about 80%, we added mesoporous silica nanomaterials loaded...

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Abstract

The invention discloses a specific targeted breast cancer cell mesoporous silicon nanometer drug loading system and a preparation method thereof. The specific targeted breast cancer cell mesoporous silicon nanometer drug loading system is characterized in that after YSA short peptides targeting an EphA2 receptor and specific D4 short peptides targeting an EGFR receptor are chemically cross-linkedon the surfaces of synthesized mesoporous silicon dioxide nanoparticles, a chemotherapeutic drug for a breast cancer is loaded in a pore passage of mesoporous silicon dioxide; through specific bindingof the YSA short peptides and the D4 short peptides to the breast cancer cell membrane high-expression EphA2 and EGFR, a double targeting effect of the drug loading MSN system is realized. The specific targeted breast cancer cell mesoporous silicon nanometer drug loading system disclosed by the invention has the characteristics of breast cancer specific targeting, active targeting, drug deliverystability and reliability and the like; the binding of the drug loading system to receptors with different high expressions on a breast cancer cell membrane is effectively improved through double targeting, so that while the anti-cancer effect is enhanced, the adverse reaction to normal cells is significantly reduced.

Description

technical field [0001] The invention relates to an MSN drug-carrying system specifically targeting the high expression of breast cancer cell membranes and a preparation method thereof, belonging to the technical field of research and development and preparation of cancer cell-targeted drugs. Background technique [0002] Breast cancer is the most common cancer in women and the second leading cause of cancer-related death in women around the world. The incidence of breast cancer is increasing in some less developed countries in South America, Africa, and Asia, due to changes in lifestyle and new screening procedures. In the United States in 2015, the estimated number of new cases was 234,190, bringing the estimated death toll to 40 730. Breast cancer, which affects one in eight to one in ten women, has reduced breast cancer deaths in developed countries, including North America and the European Union, largely due to early detection and effective systemic treatment. Chemothe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K47/04A61K31/704A61P35/00
CPCA61K31/704A61K47/02A61K47/42A61P35/00
Inventor 刘志陶自坚张晴万松张丰林
Owner 马鞍山市人民医院
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