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Efficient Gd-loaded liposome preparation and preparation method thereof

A technology of gadolinium-loaded lipids and liposomes, which is applied in preparations for in vivo tests, pharmaceutical formulations, nuclear magnetic resonance/magnetic resonance imaging contrast agents, etc., to achieve small particle size, good stability, and good sustained-release effect Effect

Inactive Publication Date: 2011-06-01
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, for a water-soluble uncharged drug, it is not easy to entrap a high-encapsulation liposome

Method used

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  • Efficient Gd-loaded liposome preparation and preparation method thereof
  • Efficient Gd-loaded liposome preparation and preparation method thereof
  • Efficient Gd-loaded liposome preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh 10g of soybean lecithin, 2.5g of cholesterol, and 0.2g of vitamin E, and dissolve them in 300ml of chloroform, remove the solvent by rotary evaporation under constant temperature and reduced pressure at 45°C to form a lipid film; add 1000ml of phosphate buffer (pH7.4) for hydration Elute the film for 3.5 hours to obtain blank liposomes; carry out high-pressure homogenization of the blank liposomes, homogenize 15 times at 50 MPa, filter and sterilize with a 0.22 micron filter membrane, and vacuum concentrate to 20 ml at room temperature to obtain Phospholipid gel. Take 1ml of phospholipid gel and mix it with 1ml of 0.8mmol / ml Gd-DTPA, and incubate at 45°C for 5 hours. Packing and sealing.

[0030] The volume average particle diameter measured by a dynamic light scattering laser particle size analyzer is 107.0nm, and its transmission electron microscope pictures and particle size distribution diagrams are shown in figure 1 and figure 2 , its in vitro sustained r...

Embodiment 2

[0034] Weigh 24g of egg yolk phospholipids, 4g of cholesterol, and 0.6g of vitamin E, and dissolve them in 300ml of chloroform and methanol (volume ratio 1:1), remove the solvent by rotary evaporation at a constant temperature and reduced pressure at 35°C to form a lipid film; add 1500ml of normal saline for hydration Elute the film for 3 hours to obtain blank liposomes; homogenize the blank liposomes under high pressure, 10 times at 80 MPa, filter and sterilize with a 0.22 micron filter membrane, and vacuum concentrate to 20 ml at room temperature to obtain phospholipids gel. Take 1ml of phospholipid gel and mix with 1ml of 0.6mmol / ml Gd-DTPA-BMA, and incubate at 45°C for 5 hours. Packing and sealing.

Embodiment 3

[0036] Weigh 15g of hydrogenated soybean lecithin, 2g of cholesterol, and 0.4g of vitamin E, and dissolve them in 300ml of absolute ethanol, remove the solvent by rotary evaporation at a constant temperature and reduced pressure at 40°C to form a lipid film; add 1000ml of phosphate buffer (pH6.8) for Hydrate and elute the film for 3 hours to prepare blank liposomes; carry out high-pressure homogenization of the blank liposomes, homogenize 6 times at 90 MPa, filter and sterilize with a 0.22 micron filter membrane, and vacuum concentrate to 20 ml at room temperature to obtain Phospholipid gel. Take 1ml of phospholipid gel and mix with 1ml of 0.4mmol / ml Gd-DTPA, and incubate at 45°C for 5 hours. Packing and sealing.

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Abstract

The invention relates to a composite for diagnosing a human body or an animal body, namely, an efficient Gd-loaded liposome preparation and a preparation method thereof. The liposome preparation is prepared from the following components in parts by weight: 30-80 parts of paramagnetic Gd contrast agent, 250-500 parts of lecithin, 50-200 parts of liposome stabilizer and 200-600 parts of buffer solution, based on the weight of metal Gd. The Gd-loaded liposome is prepared by using a phospholipid gel method, and the Gd-loaded amount of the liposome prepared by the method is high, thereby effectively delaying the retention period of the contrast agent in the body; and the liposome is good in storage stability.

Description

technical field [0001] The invention relates to a liposome preparation of a paramagnetic gadolinium contrast agent for diagnosis, which has the characteristics of high-efficiency gadolinium loading and slow release, and can be used as a contrast enhancement agent for diagnostic imaging forms such as MRI, CT, and scintigraphy. And then used for early diagnosis of tumor. Background technique [0002] Tumors are a serious threat to human health and life. Around the world, about 6 million people die from malignant tumors every year, and about 10 million people are diagnosed. The key problem facing tumor treatment is how to detect, diagnose and treat early. At present, there are a variety of tumor diagnostic techniques in imaging, such as magnetic resonance imaging, X-ray imaging, ultrasound imaging and nuclear medicine imaging. Among them, the contrast agent is used to enhance the intensity of the image, by changing the local magnetic field strength or relaxation time of the t...

Claims

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Application Information

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IPC IPC(8): A61K49/18A61K49/06A61K49/10
Inventor 钱秀珍徐云龙赵崇军戎丽娜
Owner EAST CHINA UNIV OF SCI & TECH
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