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A kind of preparation method of hectorite nanoparticles modified by TPGS

A nanoparticle and hectorite technology, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve unsatisfactory clinical treatment results, no discovery of preparation methods, high prices, etc. problems, to achieve good colloidal stability and biocompatibility, easy operation and separation, and low cost of raw materials

Active Publication Date: 2021-12-10
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there are always defects in these methods, such as large side effects, poor effect, high price, etc., and the clinical treatment results are not satisfactory.
[0004] Retrieval of domestic and foreign literature has not yet found relevant reports about a preparation method of hectorite nanoparticles modified with polyethylene glycol 1000 vitamin E succinate (TPGS)

Method used

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  • A kind of preparation method of hectorite nanoparticles modified by TPGS
  • A kind of preparation method of hectorite nanoparticles modified by TPGS
  • A kind of preparation method of hectorite nanoparticles modified by TPGS

Examples

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Effect test

Embodiment 1

[0035] A preparation method of hectorite nanoparticles modified by TPGS:

[0036]Dissolve 50mg of laponite LAP powder in 5mL of ultrapure water, and magnetically stir overnight in a water bath at 50°C to completely dissolve the LAP to obtain a transparent solution; take 1mL of an aqueous solution of APMES with a concentration of 20mg / mL, and slowly add the above LAP dropwise In the aqueous solution, and keep the temperature of the water bath at 50°C for 16 hours. After the reaction was finished, it was naturally cooled to room temperature, and the product was dialyzed for 3 days with a dialysis bag with a molecular weight cut-off of 8000-14000 (2 L of distilled water was used for each dialysis, and the water was changed 9 times in total). After dialysis, transfer the product in the dialysis bag to a 50mL EP tube and store at 4°C to obtain LM-NH modified with silane coupling agent 2 .

[0037] 10.28 mg of TPGS was dissolved in DMSO (5 mL) solution and activated with CDI (11.0...

Embodiment 2

[0042] Get the LAP obtained in embodiment 1 and comparative example 1, LM-NH 2 , LM-TPGS, LM-TPGS / DOX and LM-mPEG, LM-mPEG / DOX and other materials are diluted with ultrapure water to an appropriate concentration and used to measure surface potential and hydrodynamic diameter. The experimental results show (Table 1), the prepared LM-NH 2 , the surface potentials of LM-TPGS, LM-TPGS / DOX, LM-mPEG and LM-mPEG / DOX nanoparticles were -10.0±1.39, -20.0±1.56, -12.4±0.30, -14.0±3.86 and -11.3± 1.27mV, from the experimental results, after modifying the silane coupling agent, the potential value of hectorite nanoparticles increases due to the increase of surface amino groups, indicating that LM-NH 2 After the modification of TPGS and mPEG, the surface potential value decreased due to the consumption of the previously modified amino groups, indicating the successful modification of TPGS and mPEG. Due to the modification of substances such as APMES and TPGS, the hydrodynamic diameter of ...

Embodiment 3

[0046] Weigh the materials prepared in Example 1 and Comparative Example 1 respectively: LM-NH 2 , each 3mg of LM-TPGS and LM-mPEG carries out the test of NMR spectrum (such as figure 2 shown). By analyzing NMR spectra (such as figure 2 ), as can be seen from (a) figure, LM-NH 2 The peaks that appear at 0-1ppm prove that the silane coupling agent APMES can be connected to laponite by magnetic stirring; it can be seen from the figure (b) that -TOS and PEG in TPGS appear at about 0.9 and 3.8ppm, respectively. It can be seen from the figure (b) that the characteristic peak of hydrogen on the PEG methoxy group appeared at about 3.8ppm, which proved the successful modification of mPEG.

[0047] Weigh the materials prepared in Example 1 and Comparative Example 1 respectively: LM-NH 2 , each 2mg of LM-TPGS and LM-mPEG carries out infrared spectroscopy (such as image 3 shown) and thermogravimetric analysis (as Figure 4 shown). By analyzing the infrared spectrum (such as i...

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Abstract

The invention discloses a preparation method of TPGS-modified hectorite nanoparticles and the application of the prepared TPGS-modified hectorite nanoparticles in tumor chemotherapy and anti-tumor multidrug-resistant materials. The preparation method is as follows: dispersing laponite in ultrapure water, adding a silane coupling agent dropwise, stirring and reacting, cooling, and dialysis to obtain hectorite amide LM-NH 2 ; Dissolve TPGS in the solvent, add CDI to activate, dropwise add hectorite LM‑NH 2 React in the aqueous solution of TPGS, dialyze, obtain the hectorite nanoparticle LM-TPGS of TPGS modification; Add the doxorubicin aqueous solution dropwise in the aqueous solution of the hectorite nanoparticle LM-TPGS of TPGS modification, avoid light reaction, centrifugal washing, Get LM‑TPGS / DOX. The method of the invention is simple, and the prepared nano particles can be applied to inhibit the proliferation of drug-resistant cells, and have the potential of industrialization and commercialization.

Description

technical field [0001] The invention belongs to the field of nano drug-loaded materials and their preparation and application, in particular to a preparation method of TPGS-modified hectorite nanoparticles and its application in anti-tumor multi-drug resistance. Background technique [0002] Chemotherapy, as one of the important means of cancer treatment, has been highly concerned for a long time. However, many anti-tumor drugs have problems such as low clinical efficacy and high toxicity and side effects, and tumor multidrug resistance (Mutidrugresisitance, MDR) is the main reason for the failure of tumor chemotherapy. In clinical treatment, chemotherapy drugs are killing cancer cells. At the same time, it is often accompanied by the occurrence of MDR. The MDR phenomenon refers to the resistance of tumor cells to multiple drugs under the stimulation of an anticancer drug, and is the self-protection behavior of cancer cells stimulated by drugs. Increased drug efflux mediat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K47/69A61K31/704A61P35/00A61K31/77A61K31/355
CPCA61K47/60A61K47/6929A61K47/6949A61P35/00A61K31/355A61K31/704A61K31/77A61K2300/00
Inventor 郭睿史向阳姜婷婷
Owner DONGHUA UNIV
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