Polyethylene glycol-lactobionic acid modified aminated hectorite nano particle as well as preparation method and application thereof

A technology of amide lithium saponite and polyethylene glycol is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, organic active ingredients, etc. Material stability, improved drug release properties, and improved affinity effects

Inactive Publication Date: 2014-12-17
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, finding a suitable carrier is far from enough. Many anticancer drugs cannot pass through the cell membrane.

Method used

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  • Polyethylene glycol-lactobionic acid modified aminated hectorite nano particle as well as preparation method and application thereof
  • Polyethylene glycol-lactobionic acid modified aminated hectorite nano particle as well as preparation method and application thereof
  • Polyethylene glycol-lactobionic acid modified aminated hectorite nano particle as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] (1) Dissolve 32 mg of lactobionic acid (LA) (purchased from Sinopharm Chemical Reagent Co., Ltd.) with 20 mL of pH=6 buffer solution, add 1 mL of 1-ethyl-(3-dimethyl Aminopropyl) carbodiimide (EDC) was stirred for 0.5h, then 1mL of 10.1mg / mL N-hydroxysuccinimide (NHS) was added for activation for 3h, and 2mL of 44.20mg / mL was added slowly NH 2 -PEG-COOH (MW=2000) solution, after 72 hours of reaction, the reaction product was dialyzed in phosphate buffer with a 1000 dialysis bag for 24 hours, then dialyzed with distilled water for 48 hours, and finally the purified product was freeze-dried to obtain lactobionic acid modification Polyethylene glycol solid product (LA-PEG-COOH);

[0056] (2) Take a certain quality of LAP powder and disperse it in a certain volume of ultrapure water to prepare a dispersion with a concentration of 10 mg / mL, take 40 μL of (3-aminopropyl) dimethylethoxysilane and shake it while dripping Add 10mL LAP dispersion liquid, then place in 50 ℃ wate...

Embodiment 2

[0059] Prepare a DOX aqueous solution with a concentration of 1 mg / mL, add 2 mL of DOX aqueous solution to 2 mL of LM-PEG-LA aqueous solution with a concentration of 3 mg / mL, and react with magnetic stirring for 24 hours under the condition of avoiding light. After the reaction, the solution was transferred to a 15mL centrifuge tube, centrifuged (10min) at a rotational speed of 5000rpm, and the obtained precipitate was washed 3 times with deionized water to obtain drug-loaded nanoparticles LM-PEG-LA / DOX.

Embodiment 3

[0061]Prepare LM-PEG-LA / DOX with pH = 7.4 and pH = 5.4 buffers respectively to form a solution with a DOX concentration of 1 mg / mL, take 1 mL of the above solution into a dialysis bag, and place it in 9 mL of the same pH buffer placed in 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, 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-PEG-LA / DOX under different pH conditions in vitro was calculated. ( Figure 4 )

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Abstract

The invention relates to a polyethylene glycol-lactobionic acid modified aminated hectorite nano particle as well as a preparation method and application thereof. The preparation method of the polyethylene glycol-lactobionic acid modified aminated hectorite nano particle comprises the following steps: firstly, carrying out reaction on lactobionic acid with polyethylene glycol, wherein one end of the polyethylene glycol is an amino group, and the other end of the polyethylene glycol is a carboxyl, so that pegylated lactobionic acid is obtained; secondly, modifying hectorite with (3-aminopropyl) dimethyl ethoxy silane, so that a certain amount of amino groups are formed on the surface of the hectorite; thirdly, modifying nano clay hectorite with the pegylated lactobionic acid, so that a lactobionic acid modified functional hectorite nano composite material is obtained; the lactobionic acid modified functional hectorite nano composite material can be used for preparing a nano medicine carrying system with a lactobionic acid targeting function. The polyethylene glycol-lactobionic acid modified aminated hectorite nano particle has the advantages that stability and biological compatibility of a nano particle are improved, and a specific targeting effect on liver cancer cells highly expressed by an asialoglycoprotein receptor is realized, so that a synthesized nano medicine carrying composite material can be applied to targeted delivery of an anti-cancer drug. The preparation method of the polyethylene glycol-lactobionic acid modified aminated hectorite nano particle is simple, mild in reaction conditions and easy to operate and has an industrialization implementation 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-lactobionic acid modified hectorite amidide nanoparticle and its preparation and application. Background technique [0002] For a long time, tumors have been the number one killer that endangers human life. Tumors have the characteristics of high mortality, difficult treatment, and rapid deterioration. According to the report of the World Health Organization, there are more than 10 million new cases of cancer worldwide every year, and more than 7 million deaths, accounting for 12% of the total death toll. Tumor has become a major problem plaguing human health. With the development of social productivity and social progress, human beings have more urgent requirements for curing malignant tumors; although there are many drugs for treating tumors, many drugs have more or less defects. These two problems act speci...

Claims

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Application Information

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IPC IPC(8): A61P35/00A61K47/34A61K31/704A61K47/04A61K47/26
Inventor 史向阳郭睿陈光祥
Owner DONGHUA UNIV
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