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DSPE-PEG2000-AD-(FOL)2 as well as preparation method and application thereof

A technology of distearoyl phosphatidylethanolamine and stearoyl phosphatidylethanolamine, applied in the preparation of ultrasound contrast agents, distearoyl phosphatidylethanolamine-polyethylene glycol 2000-difolate and its preparation field, To achieve the effect of increasing particle size

Active Publication Date: 2017-05-31
SHANDONG UNIV QILU HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] It is not found in the prior art that L-2-Aminoadipic acid is used as an intermediate linking group to connect more folic acid to the surface of lipid DSPE, thereby realizing the enrichment of nanobubbles in tumor target sites

Method used

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  • DSPE-PEG2000-AD-(FOL)2 as well as preparation method and application thereof
  • DSPE-PEG2000-AD-(FOL)2 as well as preparation method and application thereof
  • DSPE-PEG2000-AD-(FOL)2 as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1: Preparation of distearoylphosphatidylethanolamine-polyethylene glycol 2000-bisfolate

[0050] The preparation method of distearoyl phosphatidylethanolamine-polyethylene glycol 2000-bisfolate comprises the steps:

[0051] (1) Synthesis of 1,2-distearoyl-SN-glycerol-3-phosphoethanolamine-polyethylene glycol 2000-N-hydroxysuccinimide

[0052] Dissolve 280 mg of 1,2-distearoyl-SN-glycerol-3-phosphoethanolamine-polyethylene glycol 2000 (carboxyl end) in anhydrous dichloromethane (8 mL), and add 17.5 mg of N-hydroxybutane imide and 62 mg of dicyclohexylcarbodiimide. The mixture was reacted in the dark at room temperature for 3 h. The resulting ethyl N,N-dichlorocarbamate was removed by filtration; the filtrate was poured into pre-cooled diethyl ether (200 mL), and the diethyl ether mixture was placed at -20°C for 4h. Filtration and drying yielded the desired product.

[0053] (2) Synthesis of 1,2-distearoyl-SN-glycerol-3-phosphoethanolamine-polyethylene glycol-...

Embodiment 2

[0061] Example 2: Preparation of double folic acid targeted ultrasound contrast agent

[0062] Weigh 0.5mg of Span 60, 0.5ml of Tween 80 into a 1.5mLEP tube, add 1mg of dipalmitoylphosphatidylcholine, 1mg of distearoylphosphatidylethanolamine-polyethylene glycol 2000-difolate, PBS The volume was reduced to 1mL, and the air was replaced by perfluoropropane gas. The centrifuge tube was placed in a constant temperature water bath and heated for 50 minutes until the lipid was completely dissolved. DiI dye was added in the dark, and the air was replaced by perfluoropropane gas again. Take it out after shaking for 90s, centrifuge at 300rpm for 3min, and take out the lower layer of liquid, which is the prepared bifolate-targeted ultrasound contrast agent.

[0063] The present invention will be further described below in conjunction with experimental examples, but not limited thereto.

[0064] Preparation of three ultrasound contrast agents with different folic acid contents:

[006...

experiment example 1

[0067] Experimental example 1: Characterization experiments of three ultrasound contrast agents with different folic acid contents

[0068] Observe the size and shape of nano-sized UCAs under a light microscope. Under a 1000× light microscope, it can be seen that the nanobubbles with different folic acid contents are spherical, uniform in particle size, uniformly dispersed without aggregation, see figure 2 . Nano laser particle size and Zeta potential analyzer were used to detect the particle size of ultrasound contrast agent. The average value of all indicators was measured three times. The particle size distribution of nanobubbles with different folic acid content was different. The particle sizes of A, B, and C groups were 129.43± 12.33nm, 244.1±35.09nm, 286.87±22.96nm, see figure 2 . The particle size of nanobubbles in the single folic acid group and the double folic acid group was significantly different from that in the blank group (both P0.05). The diameter is less...

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Abstract

The invention discloses DSPE-PEG2000-AD-(FOL)2 as well as a preparation method thereof. According to the method, 1,2-distearoyl-SN-glycero-3-phosphoethanolamine-polyethylene glycol-N-hydroxysuccinimide is synthesized firstly, lipid with double folic acid molecules is synthesized by connecting aminoadipic acid and activated amino-terminated folic acid. The invention further discloses an application of DSPE-PEG2000-AD-(FOL)2 in preparation of double folate targeted ultrasonic contrast agents. DSPE-PEG2000-AD-(FOL)2 can substantially improve the targeted combining capacity of the ultrasonic contrast agent with breast cancer MCF-7.

Description

technical field [0001] The invention belongs to the cross field of chemistry and medicine, and particularly relates to a distearoyl phosphatidylethanolamine-polyethylene glycol 2000-difolate, a preparation method thereof and an application in preparation of an ultrasonic contrast agent. Background technique [0002] The morbidity and mortality of breast cancer in women are high, and about 500,000 people die of breast cancer worldwide every year. Early detection and diagnosis of breast cancer is conducive to timely selection of corresponding treatment and reduction of mortality, which is the research goal that everyone is striving to pursue. [0003] With the rapid development of ultrasonic molecular imaging technology and bio-nanotechnology, nano-scale ultrasonic contrast agents are developing rapidly, which have high scattering properties and can significantly enhance the ultrasonic detection signal. Different from traditional ultrasound contrast agents (blood pool imaging...

Claims

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Application Information

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IPC IPC(8): C08G65/333A61K49/22
CPCA61K49/227C08G65/33396C08G2650/04
Inventor 李杰段素娟时丹丹商蒙蒙郭鲁宁松孟冬
Owner SHANDONG UNIV QILU HOSPITAL
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