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Lithium amide soapstone nano particles modified by polyethylene glycol-folic acid as well as preparation and application of lithium amide soapstone nano particles

A technology of amide lithium saponite and polyethylene glycol, which is applied in the directions of medical preparations without active ingredients, medical preparations containing active ingredients, and powder delivery.

Inactive Publication Date: 2014-11-19
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 synthesis of polyethylene glycol-folic acid-modified hectorite nanoparticles as drug carriers for anti-tumor drug delivery and tumor-targeted therapy has not been reported.

Method used

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  • Lithium amide soapstone nano particles modified by polyethylene glycol-folic acid as well as preparation and application of lithium amide soapstone nano particles
  • Lithium amide soapstone nano particles modified by polyethylene glycol-folic acid as well as preparation and application of lithium amide soapstone nano particles
  • Lithium amide soapstone nano particles modified by polyethylene glycol-folic acid as well as preparation and application of lithium amide soapstone nano particles

Examples

Experimental program
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Effect test

Embodiment 1

[0060] Dissolve 2mg of FA in 2mL DMSO, add 4mg of EDC, and stir magnetically for 4 hours. Add slowly containing 2mg NH 2 - 2 mL of DMSO solution of PEG-COOH (MW=2000), reacted with magnetic stirring for 3 days. After the reaction, all the obtained PEG-FA solution was transferred to a dialysis bag with a molecular weight cut-off of 8000-14000. Put the dialysis bag into a beaker filled with 2L of deionized water for dialysis. The dialysis lasts for 3 days, and the water is changed 3-4 times a day. After the dialysis, the product in the dialysis bag was transferred to a 15mL centrifuge tube for freeze-drying to obtain PEG-FA powder.

[0061] Dissolve mPEG-COOH (MW=2000) or PEG-FA powder in DMSO to obtain a solution with a concentration of 2 mg / mL. 2.2 mg of EDC was added thereto and magnetically stirred for 3 hours. Slowly add the prepared hectorite LM-NH with a concentration of 4mg / mL 2 Aqueous solution 1mL, magnetic stirring reaction for 3 days. After the reaction, all th...

Embodiment 2

[0063] Take 1 mL of LM-mPEG with a concentration of 3 mg / mL and 1 mL of LM-PEG-FA with a concentration of 3 mg / mL in aqueous solution, add 1 mL of DOX aqueous solution with a concentration of 1 mg / mL respectively, and react with magnetic stirring for 24 hours under the condition of avoiding light. After the reaction, the solutions were transferred to 15mL centrifuge tubes, centrifuged at 8000rpm (5min), and the obtained precipitate was washed 3 times with deionized water to obtain drug-loaded nanoparticles LM-mPEG / DOX and LM -PEG-FA / DOX.

Embodiment 3

[0065] Dissolve LM-mPEG / DOX and LM-PEG-FA / DOX with pH=7.4 and pH=5.4 buffers, respectively, to a concentration of 1 mg / mL (concentration of LM-mPEG / DOX or LM-PEG-FA / DOX) Take 1mL of the solution, put it into a dialysis bag for fixation, put it in a container containing 9mL of buffer solution with different pH, and place it on a shaker at 37°C for shaking. 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, and then add 1mL of the corresponding buffer solution to the outside of the dialysis bag. The absorbance value at 480nm of the dialysate taken out was measured, and the release curve of DOX released from LM-mPEG / DOX and LM-PEG-FA / DOX under different pH conditions in vitro was calculated. ( Figure 4 )

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Abstract

The invention relates to lithium amide soapstone nano-particles modified by polyethylene glycol-folic acid as well as preparation and application of the lithium amide soapstone nano particles. Lithium amide soapstone is lithium soapstone modified by (3-aminopropyl) ethoxydimethyl-silane APMES; the mol ratio of polyethylene glycol to folic acid is (1:0.4)-(1:0.8); and the mass percentage of polyethylene glycol-folic acid is 45-55%. The preparation disclosed by the invention comprises the following steps of dissolving folic acid in a solvent, adding 1-(3-dimethylaminopropyl)-3-ethyl carbodiimide hydrochloride EDC, stirring to obtain mixed solution, adding the mixed solution into polyethylene glycol solution drop by drop, stirring in 2-3 d, dialyzing, freezing, drying, and obtaining polyethylene glycol-folic acid PEG-FA; and adding EDC into PEG-FA solution, stirring for 2-4 h, adding into aqueous solution of the lithium amide soapstone nano particles drop by drop, magnetically stirring in 2-3 d and dialyzing, thereby obtaining the lithium amide soapstone nano particles modified by polyethylene glycol-folic acid. The lithium amide soapstone nano particles modified by polyethylene glycol-folic acid are applied to drug load, have the advantages of simple preparation method, moderate condition and wide application range, and have good market prospect.

Description

technical field [0001] The invention belongs to the field of nano drug-loaded materials and their preparation and application, in particular to a polyethylene glycol-folic acid modified hectorite amidide nanoparticle and its preparation and application. Background technique [0002] Cancer is considered to be one of the major challenges facing mankind in the 21st century. In the process of using chemical drugs to treat tumors, anticancer drugs have problems such as poor water solubility, short retention time at the lesion site, and inability to specifically recognize tumor cells, which will have strong toxic and side effects on the human body, and cannot effectively realize the effect of drugs on tumors. lethal effect. Therefore, the development of a carrier material with tumor-targeting effect to realize drug loading, controlled release and targeted therapy is a research hotspot in nanomedicine at present. Clay-based nanoparticles, such as Laponite (LAP), not only have go...

Claims

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Application Information

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IPC IPC(8): A61K47/46A61K31/704A61K9/14A61P35/00
Inventor 史向阳吴一伦郭睿
Owner DONGHUA UNIV
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