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Folic-acid-modified laponite nanometer particle, preparation thereof and applications thereof

A nanoparticle and hectorite technology, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., to achieve the effect of improving inhibition and broad application prospects

Inactive Publication Date: 2014-07-09
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] According to the relevant literature, it can be found that the study of synthetic folic acid-modified LAP as a drug carrier for anti-tumor drug delivery and tumor-targeted therapy has not been reported yet.

Method used

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  • Folic-acid-modified laponite nanometer particle, preparation thereof and applications thereof
  • Folic-acid-modified laponite nanometer particle, preparation thereof and applications thereof
  • Folic-acid-modified laponite nanometer particle, preparation thereof and applications thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0057] Dissolve 50mg of LAP powder in 5mL of ultrapure water, stir magnetically in a water bath at 50°C to completely dissolve LAP to obtain a transparent solution, take 1mL of an aqueous solution of APMES with a concentration of 20mg / mL, slowly add it dropwise to the above aqueous solution of LAP, and keep The temperature of the water bath was 50°C and the reaction was carried out for 16 hours. After the reaction, all the obtained solution was transferred to a dialysis bag with a cutoff analysis volume of 8000–14000. Put the dialysis bag into a beaker filled with 2L deionized water for dialysis. The dialysis lasts for 2-4 days, and the water is changed 3-4 times a day. 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 .

[0058] Dissolve 2.4mg FA in 4mL DMSO, add 5.2mg EDC, and stir magnetically for 4 hours. Take 4 mL of LM-NH with a concentration of 6.95 mg / mL 2 Aqueous soluti...

Embodiment 2

[0060] Take 3 mL of LM-NH with a concentration of 6.95 mg / mL 2 aqueous solution, and 3 mL of LM-FA aqueous solution with a concentration of 2.4 mg / mL were added to 6.95 mL and 2.4 mL of DOX aqueous solutions with a concentration of 1 mg / mL, respectively, and the reaction was carried out by magnetic stirring for 24 hours. After the reaction, the solutions were transferred to 15mL centrifuge tubes, centrifuged at 8000rpm (5min), and the obtained precipitate was washed with deionized water for 3 times to obtain drug-loaded nanoparticles LM-NH 2 / DOX and LM-FA / DOX.

Embodiment 3

[0062] LM-NH 2 / DOX and LM-FA / DOX were dissolved in pH=7.4 and pH=5.4 buffers to a concentration of 1mg / mL (LM-NH 2 / DOX or LM-FA / DOX concentration) solution, take 1mL into a dialysis bag for fixation, place it in a container containing 9mL of buffer with different pH, and place it on a shaker at 37°C. Samples were taken every 2 hours in the first 12 hours, and samples were taken every 24 hours thereafter. Take 1mL of the liquid outside the dialysis bag each time, measure its absorbance at 480nm, and then add 1mL of the corresponding buffer solution to the outside of the dialysis bag. Using this method to obtain DOX from LM-NH under different pH conditions in vitro 2 / DOX and LM-FA / DOX release profiles.

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Abstract

The invention relates to a folic-acid-modified laponite nanometer particle, preparation thereof and applications thereof. Laponite is modified by utilization of a silane coupling agent. The weight ratio of the laponite (LAP) to the silane coupling agent is 5:1-5:4. The weight percentage of the silane coupling agent and folic acid is 3.01-3.34%. The preparation includes: a step of, under stirring, adding dropwise an aqueous solution of the silane coupling agent into an aqueous solution of the laponite (LAP), reacting at 45-60 DEG C for 12-16 h and dialyzing to obtain aminated laponite LM-NH2; a step of dissolving the folic acid into a solvent, adding N-(3-Dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride EDC, and uniformly stirring to obtain a mixed solution; and a step of adding dropwise the aqueous solution of the aminated laponite LM-NH2 into the mixed solution, stirring for 2-3 d, and dialyzing. The laponite nanometer particle is used for loading medicines. The preparation has characteristics of simple method, mild reaction conditions and easy operation and has good prospect of industrial implementation.

Description

technical field [0001] The invention belongs to the field of nano drug-loaded materials and their preparation and application, in particular to a folic acid-modified hectorite nanoparticle and its preparation and application. 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, which have become the bottleneck in cancer drug treatment. Due to the inability to control the concentration of anti-tumor drugs on the tumor site, it will cause unnecessary damage to the patient's normal tissues and organs, and even threaten the patient's life. In recent years, the use of nanocarriers to load anti-tumor drugs can not only improve drug solubility, increase drug stability, and achieve drug sustained release, but also greatly change the distribution and distribution of drugs in the body by vir...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/22A61K47/04A61K31/704A61P35/00
Inventor 史向阳吴一伦郭睿
Owner DONGHUA UNIV
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