Lipidosome for magnetic resonance imaging of acute pancreatitis, and preparation and application of same

A technology for magnetic resonance imaging and acute pancreatitis, applied in liposome delivery, preparations for in vivo tests, emulsion delivery, etc., can solve the problems of different evaluation times, achieve good imaging, less toxic effects on normal tissues, Good biological targeting effect

Pending Publication Date: 2018-06-01
上海舜纳生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current clinical diagnosis and scoring system has certain limitations. Since the researchers began to evaluate the severity and prognosis of AP in the 1960s, multiple clinical objective evaluation criteria and pathological changes of the pancreas have emerged. However, the fo...

Method used

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  • Lipidosome for magnetic resonance imaging of acute pancreatitis, and preparation and application of same
  • Lipidosome for magnetic resonance imaging of acute pancreatitis, and preparation and application of same
  • Lipidosome for magnetic resonance imaging of acute pancreatitis, and preparation and application of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Synthesis of targeted lipid material Man-PEG-DSPE

[0029] Mix 10 μmol of 1,2-distearoyl-SN-glycerol-3-phosphoethanolamine-N-amino (DSPE-PEG-NH2, purchased from AVANTI, USA) with 40 μmol of 2-imino-2-methoxy Ethylethyl-1-thiomannoside (IME-thiomannoside, purchased from Carbosynth, USA) was added to deionized water, reacted at room temperature for 8 hours, added 10 μl of 1M acetic acid to stop the reaction, and dialyzed with 3000 molecular weight The bag (purchased from Millipore, USA) was dialyzed for 12 hours, and the solution in the dialysis bag was further separated through a Sephadex chromatography column (Pharmacia) to obtain a Man-DSPE-PEG solution, which was freeze-dried to obtain 12.2 mg.

Embodiment 2

[0030] Example 2: Preparation of Nanoliposomes Rich in (DTPA(Gd))

[0031] Weigh 6 mg of Man-PEG-DSPE prepared in Example 1, 15 mg of 1,2-dipalmitoyl-sn-glycerol-3-phosphoethanolamine-diethylenetriaminepentaacetic acid gadolinium dimeglumine (DPPE- DTPA (Gd), purchased from American AVANTI Company) and 10 mg of cholesterol were fully dissolved in 200 μl of absolute ethanol, and injected into 2 ml of ionic aqueous solution at a temperature of 50 ° C at a rate of 1 ml / min, and after magnetic stirring for 30 min, the obtained The solution was sequentially squeezed through polycarbonate membranes with pore sizes of 400nm, 200nm, 100nm, and 50nm (purchased from Millipore, USA) 20 times each; 5.2ml of liposomes with uniform particle size were collected through a Sephadex gel column.

Embodiment 3

[0032]Example 3: Preparation of Gd Nanoliposome Man-Gd-Lip Targeted by Pancreatitis Macrophages

[0033] 5ml of nanoliposomes rich in (DTPA(Gd)) prepared in Example 2, after rapidly raising the temperature of the collected liposome solution to 55°C, adding 2mg of Man-PEG-DSPE, dissolved and standing for 2 hours, The macrophage-targeted Man-Gd-Lip was collected through a Sephadex gel column; after freeze-drying, 11.2 mg of solid powder was obtained.

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Abstract

The invention provides a nano-lipidosome for magnetic resonance imaging of acute pancreatitis, wherein a lipid material in the nano-lipidosome includes a mannitol-modified distearyl phosphatidyl ethanolamine-polyethylene glycol copolymer and cholesterol, and the nano-lipidosome is rich in a lipid conjugate of a MRI T1 contrast agent diethylenetriaminepentaacetic acid gadolinium bismeglumine (DTPA(Gd)). The nano-lipidosome is targeted to a mannitol receptor on the surface of inflammatory macrophages, and achieves effective determination between normal pancreas and pancreas in acute pancreatitisby enhancing the MRI T1 signal of the macrophages at the lesion of the acute pancreatitis. Furthermore, by means of intensity change of the T1 signal value, the difference of number of the macrophages at the lesion can be determined, so that the nano-lipidosome can effectively distinguish lesser and severe acute pancreatitis.

Description

technical field [0001] The present invention relates to a liposome for magnetic resonance imaging of acute pancreatitis, in particular to a nano-liposome targeting inflammatory macrophages rich in T1 contrast agent DTPA (Gd), and Preparation and application. Background technique [0002] The incidence of acute pancreatitis (AP) is increasing year by year, seriously affecting people's work and quality of life. The morbidity and mortality of AP are high. Mild acute pancreatitis (MAP) is self-limiting, but 20%-30% can develop into severe acute pancreatitis (SAP). Therefore, early diagnosis, typing, and assessment are particularly important for mastering the progress of AP, timely and effective intervention, and judging the prognosis. However, the current clinical diagnosis and scoring system has certain limitations. Since the researchers began to evaluate the severity and prognosis of AP in the 1960s, multiple clinical objective evaluation criteria and pathological changes of...

Claims

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Application Information

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IPC IPC(8): A61K49/10A61K49/18A61K49/12
CPCA61K49/105A61K49/126A61K49/1812
Inventor 陈怀文高洁董银梅郝强张莹莹尹川田冰杨冬梅贺智明王凤英
Owner 上海舜纳生物科技有限公司
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