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Glycyrrhetinic acid-modified tanshinone-loaded phase-transition ultrasonic contrast agent and preparation method thereof

An ultrasonic contrast agent, glycyrrhetic acid technology, applied in the field of medical drugs, can solve problems such as poor development effect, and achieve the effects of less time-consuming, good biocompatibility, and simple synthesis process

Inactive Publication Date: 2017-05-31
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide a new glycyrrhetinic acid-modified tanshinone-loaded solution for the problems that the gaseous microbubbles have a large particle size (micron level) and cannot penetrate the vascular endothelial space and the liquid fluorocarbon PFOB nanospheres have poor aggregation and development effects. Phase-change nano-ultrasound contrast agent and preparation method thereof

Method used

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  • Glycyrrhetinic acid-modified tanshinone-loaded phase-transition ultrasonic contrast agent and preparation method thereof
  • Glycyrrhetinic acid-modified tanshinone-loaded phase-transition ultrasonic contrast agent and preparation method thereof
  • Glycyrrhetinic acid-modified tanshinone-loaded phase-transition ultrasonic contrast agent and preparation method thereof

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Experimental program
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Embodiment 1

[0027] 1. Preparation of glycyrrhetinic acid active ester

[0028] Weigh 0.564g of glycyrrhetinic acid, 0.115g of NHS and 0.250g of DCC and dissolve them in tetrahydrofuran (THF), stir at room temperature in the dark for 24 hours, filter to remove the white by-products after the reaction is completed, concentrate the filtrate, wash with ether, and dry the existing licorice. Acid active ester.

[0029] 2. Preparation of Glycyrrhetinic Acid-Modified Phospholipid Polyethylene Glycol Complex

[0030] Weigh 5mg DSPE-PEG2000-NH 2 Dissolve 2 mg of glycyrrhetinic acid active ester in dichloromethane, stir overnight at room temperature to obtain glycyrrhetinic acid-modified phospholipid-polyethylene glycol complex (DSPE-PEG2000-GA), evaporate to dryness, seal and store at -20°C spare.

[0031] 3. Preparation of blank phase-change nano-ultrasound contrast agent

[0032] Weigh 7mg of DPPC, 1.5mg of DSPE-PEG2000 and 2mg of cholesterol in a 100mL round bottom flask, add 5mL of dichloro...

Embodiment 2

[0037] 1. Glycyrrhetinic acid-modified tanshinone-loaded phase-change nano-ultrasound contrast agent in vitro heating-induced phase-change microscope observation

[0038] Dilute the prepared glycyrrhetinic acid-modified tanshinone-loaded phase-change nano-ultrasound contrast agent suspension to a certain multiple, drop it on a glass slide, place it in the middle of the heating plate, and use an inverted microscope to observe the liquid that occurs at different temperatures—— Gas phase change. Phase transition results see image 3 , the results showed that before heating, the lipid nanospheres had no phase transition, but with the increase of temperature, a liquid-gas phase transition occurred gradually, at 37°C, a small amount of bubbles were generated, and when heated to 50°C, the bubbles became more and more many. When the bubbles increase to a certain volume, they will collapse or merge.

[0039] 2. Ultrasonic imaging observation of glycyrrhetinic acid-modified tanshinon...

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Abstract

The invention discloses a glycyrrhetinic acid-modified tanshinone-loaded phase-transition ultrasonic contrast agent and a preparation method thereof. The method includes the preparation of glycyrrhetinic acid active ester, the preparation of lipid coating and the preparation of nanospheres by adopting an ultrasonic cell disruptor to perform ultrasonic processing. The grain size of the lipid nanospheres prepared by the invention is small, the average grain size is about 310nm, and passive targeting can be implemented by a tumor site EPR (Enhanced Permeability and Retention) effect. Moreover, glycyrrhetinic acid modification can also realize active targeting to the liver, consequently, the toxic and side effects of the preparation can be decreased, and the curative effect of the drug can be enhanced. On the other hand, the nanospheres which wrap low-boiling point liquid fluorocarbon with lipid as coating have good biocompatibility. Under certain conditions, enhanced ultrasonography can be performed by liquid-gas phase transition, the theranostics of tumors can be implemented after the anticancer drug tanshinone is loaded, consequently, intermediate links can be reduced, efficiency can be greatly increased, and the contrast agent has a broad clinical application prospect.

Description

technical field [0001] The invention relates to the field of medical medicine, in particular to a glycyrrhetinic acid-modified tanshinone-loaded phase-change nano-ultrasonic contrast agent and a preparation method thereof. Background technique [0002] Salvia miltiorrhiza is one of the traditional Chinese medicines commonly used in TCM clinics. It has the effects of promoting blood circulation, removing blood stasis, regulating menstruation, relieving pain, and calming the nerves. Tanshinone has a high content in Danshen and is the main active ingredient of Danshen. Its pharmacological effects are extremely extensive, including not only antioxidant effects, cardiovascular pharmacological effects, sex hormone effects, cerebrovascular pharmacological effects, antibacterial and anti-inflammatory effects, but also obvious anti-tumor effects. effect. Its anti-tumor mechanism includes inhibiting tumor growth and proliferation, inhibiting tumor invasion and migration, and synergis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/22A61K47/28A61K9/16A61K31/58A61P35/00
CPCA61K49/221A61K9/1617A61K31/58A61K49/227
Inventor 张良珂张萍
Owner CHONGQING MEDICAL UNIVERSITY
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