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Nanometer drug carrier (bevacizumab medicated-SiO2@LDH (sodium dioxide @ double hydroxide)) with active tumor targeting function, preparation method and application

A nano-drug carrier, bevacizumab technology, applied in the direction of anti-tumor drugs, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of lack of active tumor targeting

Inactive Publication Date: 2016-10-12
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In recent years, the targeting properties of targeted nanotransmission carriers that have been widely studied are mostly passive targeting caused by the high permeability and retention (EPR effect) of solid tumors different from normal tissue structures. An ability to actively target tumors

Method used

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  • Nanometer drug carrier (bevacizumab medicated-SiO2@LDH (sodium dioxide @ double hydroxide)) with active tumor targeting function, preparation method and application
  • Nanometer drug carrier (bevacizumab medicated-SiO2@LDH (sodium dioxide @ double hydroxide)) with active tumor targeting function, preparation method and application
  • Nanometer drug carrier (bevacizumab medicated-SiO2@LDH (sodium dioxide @ double hydroxide)) with active tumor targeting function, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: (1) SiO 2 preparation of

[0029] Dissolve 0.985g CTAB in 100mL methanol, add 120mL double distilled water, mix well and add 0.57mL1mol / L NaOH solution under the liquid surface; add 0.325mLTEOS dropwise, stir for 8 hours, and centrifuge to collect the precipitate; use double distilled water-absolute ethanol for the precipitate After washing, resuspend with absolute ethanol (15mL), transfer to a hydrothermal tank, add double distilled water (10mL), 1,3,5-trimethylbenzene (10mL), mix well, and place in a hydrothermal tank at 140°C Heat water for 4 days; take it out after 4 days, wash the precipitate collected by high-speed centrifugation with absolute ethanol-double distilled water, resuspend with absolute ethanol and transfer it to a three-necked flask, add concentrated hydrochloric acid (v ethanol / v hydrochloric acid=5: 1), heating to reflux for 6 hours; after the reflux is completed, high-speed centrifugation collects the precipitate, and the precipitate is...

Embodiment ２

[0038] Example 2: SiO 2 @LDH-Bev-Dox Cytotoxicity Study

[0039] (1) MTT

[0040] 96-well plate plated at a density of 5000 per well, 37°C, 5% CO 2 After culturing for 18-24 hours under certain conditions, use the medium to prepare SiO according to the concentration of Dox 2 @LDH-Dox, SiO 2 @LDH-Bev-Dox and Dox solution, the concentration is 1, 5, 10 μg / mL, after culturing for 24 hours, add 20 μL MTT solution (5 mg / mL prepared in PBS) to each well, keep in the dark for 4 hours, add 150 μL DMSO to each well, and keep in the dark Shake for 15 minutes, and measure the OD value with a microplate reader.

[0041] (2) Cell cycle

[0042] Cells according to cell density 1.5*10 5 cells / mL inoculated in 12-well plate, 5% CO 2 , Cultivate at 37°C to a fusion density of 70%, and prepare Dox and SiO in the culture medium 2 @LDH-Dox, SiO 2 @LDH-Bev-Dox solution, so that the Dox concentration is 1 μg / mL, added to a 12-well plate, leaving two blank control wells, continued to cultur...

Embodiment 3

[0043] Example 3: In vitro targeting evaluation

[0044] cells according to cell density 10 5 cells / mL inoculated in a confocal small dish, incubated at 5% CO2, 37°C for 16-18 hours to make the cells adhere to the wall; prepared three kinds of materials, so that the final concentration of the drug added was 1 μg / mL; sucked off the culture medium, and washed with PBS Wash three times, fix with 4% paraformaldehyde at room temperature in the dark for 15 minutes, absorb the fixative, wash three times with PBS, stain with DAPI at room temperature in the dark for 15 minutes, absorb the dye solution, wash with PBS three times, add 500 μL PBS, and detect by laser confocal .

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Abstract

The invention relates to a nanometer drug carrier (bevacizumab medicated-SiO2@LDH (sodium dioxide @ double hydroxide)) with an active tumor-targeting function, a preparation method and an application. The nanometer drug carrier uses mesoporous silica as a core, an outer layer is coated with magnesium-aluminum LDH, and the surface is connected with bevacizumab to form a nanometer compound. The nanometer drug carrier can be carried with a treatment drug; the purpose of tumor-targeting treatment is realized by recognizing the bevacizumab specificity and combining with the characteristics of VEGF (vascular endothelial growth factor) which is excessively secreted by tumors. The nanometer drug carrier has the advantages that the safety, active targeting property and drug carrying effect are higher; the synthesis method is simple, the cost is economic, and the application prospect in tumor-targeting treatment is broad.

Description

technical field [0001] The invention relates to a nano-drug carrier with active tumor targeting-bevacizumab-mediated SiO 2 @LDH, preparation method and application. Background technique [0002] At present, with the increase in the incidence of tumors, the threat of cancer to humans has become increasingly prominent. The traditional treatment methods for cancer mainly include surgery, chemotherapy and radiotherapy, but these methods can not achieve the expected effect on the treatment of malignant tumors, and are often accompanied by serious negative effects. New methods are still needed to solve the problem. [0003] Since the existing traditional treatment methods and the newly proposed biological treatment represented by gene therapy and immunotherapy are not specific treatments for tumors, they will inevitably cause damage to normal cells, tissues and organs, and reduce the The effect of the treatment. To solve this problem, the concept of tumor-targeted therapy has b...

Claims

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Application Information

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IPC IPC(8): A61K39/395A61K45/06A61K47/04A61K47/02A61P35/00
Inventor 汪世龙朱融融王兆琪
Owner TONGJI UNIV
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