Ultrasonic preparation method of targeted polyethylene glycol nanoparticle drug carrier and application thereof

A polyethylene glycol and nanoparticle technology, applied in the fields of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of difficulty in preparing polyethylene glycol particles, complex and harsh synthesis conditions, time-consuming and labor-intensive, etc. The effect of high monomer conversion efficiency, improved specific interaction, and short polymerization time

Active Publication Date: 2019-12-31
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The silica template method has various shapes and is easy to control the size, but it needs to use dangerous substances such as hydrofluoric acid when removing the template
Calcium carbonate and polystyrene templates are relatively easy to remove, but difficult to use to make small-sized PEG particles
For the bulk phase polymerization method, the synthesis conditions are usually complex and harsh, time-consuming and labor-intensive, and the reaction process generally introduces some organic substances such as catalysts, which have certain biological toxicity for subsequent applications.

Method used

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  • Ultrasonic preparation method of targeted polyethylene glycol nanoparticle drug carrier and application thereof
  • Ultrasonic preparation method of targeted polyethylene glycol nanoparticle drug carrier and application thereof
  • Ultrasonic preparation method of targeted polyethylene glycol nanoparticle drug carrier and application thereof

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Experimental program
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Effect test

Embodiment 1

[0072] Cisplatin prodrug molecule c,c,t-[Pt(NH 3 ) 2 Cl 2 (OH)(O 2 CCH 2 CH 2 CO 2 H)] synthesis,

[0073] (1) Combine cisplatin with H 2 o 2 Mix according to the molar ratio of 1:10, add ultrapure water, react for 1 hour, and the precipitate obtained after the reaction is washed with cold water for 3 times, ethanol for 3 times, ether for 3 times, and vacuum dried to obtain c,c ,t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ];

[0074] (2) put c,c,t-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ] mixed with succinic anhydride at a molar ratio of 1:10, added to DMSO, reacted for 12 hours at a temperature of 40°C, DMSO was freeze-dried, added acetone to precipitate the product, washed 3 times with acetone, washed 3 times with ether, and dried To obtain cisplatin prodrug molecules;

[0075] The prepared cisplatin prodrug molecule c,c,t-[Pt(NH 3 ) 2 Cl 2 (OH)(O 2 CCH 2 CH 2 CO 2 H)] 1 The H NMR spectrum is as figure 1 shown.

[0076] ACLT-PEG 5k -RGD was prepared as follows: ACLT-PEG 5k -NH...

Embodiment 2

[0079] The preparation of targeted polyethylene glycol nanoparticles, the molecular weight of polyethylene glycol is 2k, the steps are as follows:

[0080] ACLT-PEG 2k (138mg, 0.069mmol), AEMA (4.5mg, 0.0345mmol) and ACLT-PEG 5k -RGD (57.5mg, 0.0115mmol) was dissolved in 1mL ultrapure water, and nitrogen gas was blown for 30min to remove oxygen. The reaction system was ultrasonically polymerized under the conditions of 40° C., 40 W, and 412 kHz for 20 minutes. Add 9 mL of cold water to the reaction system to terminate the polymerization reaction. The reaction solution was transferred to a dialysis bag for dialysis for 2 days, and then freeze-dried into powder to obtain targeted polyethylene glycol nanoparticles.

[0081] The Zeta potential, TEM image, and AFM image of the obtained targeted polyethylene glycol nanoparticles are shown in image 3 , 4 , 5 shown.

[0082] The GPC test shows that the molecular weight of the nanoparticles is about 1300kDa, and the hydration ki...

Embodiment 3

[0084] The preparation of drug-loaded system, the steps are as follows:

[0085] Take by weighing cisplatin prodrug molecule 20mg (0.046mmol), DMTMM 19.09mg (0.069mmol) and the polyethylene glycol nanoparticle PEG NPs 30mg of embodiment 2, polyethylene glycol molecular weight is 2k, dissolves in 1mL PBS (10mM, pH 7.4) buffer solution, stirred at room temperature for 24 h. After the reaction, the reaction solution was dialyzed for 2 days to remove unreacted cisplatin prodrug molecules and catalyst DMTMM. Freeze-dried into powder to obtain targeted polyethylene glycol nano-drug carriers (Pt-loaded PEG-RGD NPs) loaded with cisplatin prodrug molecules.

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Abstract

The invention relates to an ultrasonic preparation method of a targeted polyethylene glycol nanoparticle drug carrier and an application thereof, the targeted polyethylene glycol nanoparticles are prepared by adopting an ultrasonic polymerization method, and the method is free of introduction of an initiator and a catalyst, and is especially suitable for preparation of a biological sample. Meanwhile, the ultrasonic polymerization method is short in polymerization time, the monomer conversion efficiency is high, the targeted polyethylene glycol nano-drug carrier (Pt-loaded PEG-RGD NPs) loaded with the cisplatin prodrug molecule is obtained by loading the cisplatin prodrug molecule on the basis of the characteristic of a tumor microenvironment, so that the cisplatin of the anti-cancer drug molecule can be controllably released on the basis of the characteristic of the tumor microenvironment, and the toxic and side effects of the anti-cancer drug molecule are reduced.

Description

technical field [0001] The invention relates to an ultrasonic preparation method and application of a targeted polyethylene glycol nanoparticle drug carrier, belonging to the technical field of polymer materials. Background technique [0002] Cancer is a worldwide scientific problem in the 21st century, and it is also one of the diseases that seriously affect human life and health in the world today. The common treatment methods include surgery, radiotherapy, chemotherapy, gene therapy and immunotherapy. Chemotherapy, as an important cancer treatment method, has a very good application in tumor control and postoperative treatment. However, traditional anticancer drugs have disadvantages such as low drug utilization rate, high toxicity and side effects, and no specific recognition. In recent years, different types of drug carriers (such as micelles, capsules, dendrimers, inorganic nanoparticles, proteins and hydrogels, etc.) have been gradually developed. The design of the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/60A61K47/64A61K33/24A61P35/00
CPCA61K47/6935A61K47/64A61K33/24A61P35/00
Inventor 崔基炜高至亮
Owner SHANDONG UNIV
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