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Brain targeted liposome preparation of <99m>Tc tumor imaging medicament and application thereof

A technology targeting liposomes and liposome preparations, applied in the direction of radioactive carriers, radioactive physical shapes, etc., to achieve the effect of facilitating drug loading and reducing the possibility

Inactive Publication Date: 2010-12-22
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to the literature search, there is no 99m Research report on the application of Tc imaging drug liposome preparation in brain tumors

Method used

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  • Brain targeted liposome preparation of &lt;99m&gt;Tc tumor imaging medicament and application thereof
  • Brain targeted liposome preparation of &lt;99m&gt;Tc tumor imaging medicament and application thereof
  • Brain targeted liposome preparation of &lt;99m&gt;Tc tumor imaging medicament and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Preparation process and toxicity of active targeting liposomes with bradykinin analogue RMP-7 as the targeting molecule

[0016] Take an appropriate amount of DSPE-PEG-NHS and RMP-7 and dissolve them in 0.1mol / L HEPES buffer solution; then slowly add DSPE-PEG-NHS to the RMP-7 solution in a 4°C freezer, and stir slowly. After reacting at 4°C for 12 hours, an excess of 0.1 mol / L glycine was added to terminate the reaction. The reaction solution was freeze-dried at -40°C and 0.22 mbar for 24 hours to obtain DSPE-PEG-RMP-7, and RMP-7 was completely reacted without residue. Dissolve DSPE-PEG-RMP-7 with physiological saline, slowly drop it into liposomes, stir slowly, and the hydrophobic end of DSPE-PEG-RMP-7 will be automatically inserted into the lipid membrane of liposomes by hydrophobic interaction to form Actively targets liposomes.

[0017] SD rats were intravenously injected with RMP-7 once a day for 14 days, and the mortality rate of the rats was 33%. Simi...

Embodiment 299m

[0018] Example 2 99m Tc drugs (with 99m TcN-NOET is an example) liposome preparation process

[0019] Take appropriate amount of soybean lecithin SPC, cholesterol CHl and appropriate amount according to the optimized prescription 99m The Tc drug is dissolved in a suitable oil phase, and evaporated under reduced pressure at 25-30° C. to form a film. Then add a certain amount of physiological saline to make it hydrated, and disperse into a uniform liposome suspension after ultrasonication for 5 minutes. obtained by this method 99m The common liposome of Tc drug is characterized as a transparent liquid with blue opalescence, an encapsulation rate of 99%, and an average particle diameter of less than 30nm. If you add appropriate amount of DSPE-PEG-RMP-7 and DSPE-PEG to ordinary liposomes and incubate for 1 hour, you will get 99m TcN-NOET brain-targeted liposome is also characterized as a transparent liquid with blue opalescence, an encapsulation rate of 99%, and an average pa...

Embodiment 399m

[0024] Example 3 99m Tc drugs (with 99m TcN-NOET as an example) liposome intravenous administration for brain tumor diagnosis

[0025] 1. 99m Distribution of TcN-NOET liposome in the brain tissue of mice administered intravenously

[0026] 1. Experimental method:

[0027] 90 ICR male mice (body weight 20g) were divided into 3 groups, followed by free 99m TcN-NOET, 99m TcN-NOET liposome ( 99m TcN-NOET-L) and 99m TcN-NOET actively targets liposomes ( 99m TcN-NOET-SSL-T) group. After anesthetized with 15% urethane, 0.1 ml was administered into the tail vein. Blood was collected from the retroocular venous plexus at 5, 15, 30, 60 and 120 minutes after administration, respectively. Then the peristaltic pump is used to perfuse the heart with normal saline at a flow rate of 2mL / min, and then the right atrial appendage is cut open and bled to eliminate the influence of the residual drug in the brain capillaries on the distribution of the brain tissue, and to accurately evalu...

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Abstract

The invention discloses a brain targeted liposome preparation of a <99m>Tc tumor imaging medicament and application thereof. In the invention, the idea that an active brain targeted liposome entraps the <99m>Tc tumor imaging medicament is put forward, and the brain targeted liposome preparation of the <99m>Tc tumor imaging medicament is prepared by a fast film dispersion method, wherein liposome has the entrapment rate of over 99 percent, the particle size of less than 30 nm and a structure shown in figure 1. Phospholipid is dispersed in water to form single-layer or multi-layer microcapsules; the liposoluble <99m>Tc medicament is inserted into a bimolecular lipid membrane; and a bradykinin analogue RMP-7 is spread on the surface of the liposome as an active brain targeted directing molecule. Mouse tissue distribution experiments show that the preparation greatly improves the capability of the <99m>Tc medicament in passing through BBB; the SPECT imaging and self-development results of a model of mice with C6 brain gliomas show that the active targeted liposome preparation can realize the early diagnosis of brain tumors when applied to the <99m>Tc tumor imaging medicament; and the brain targeted liposome preparation belongs to the technical field of radiopharmacy and medicinal preparations.

Description

technical field [0001] The present invention relates to a 99m The brain-targeted liposome preparation of the Tc tumor imaging drug and its application in human and animal organ imaging, especially in the early diagnosis of brain tumors, belong to the technical field of radiopharmaceuticals and pharmaceutical preparations. Background technique [0002] Epidemiological studies have shown that the mortality rate of cancer patients in my country is on the rise. Early diagnosis and treatment will bring more chances of cure and better results for cancer patients. Non-specific tumor imaging agents commonly used in clinical practice include 99m Tc-methoxy isobutyl isonitrile ( 99m Tc-MIBI), 99m Tc(V)-sodium dimercaptosuccinate (DMSA), 67 Ga-citrate (citrate), 201 TlCl, etc. [0003] Currently, 85% of nuclear medicine clinical diagnostic drugs are 99m Tc-radiopharmaceutical. However, so far, there has not been a 99m The Tc-labeled brain tumor imaging agent can be applied to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/08A61K51/12A61K103/10
Inventor 贾红梅谢英郑婷婷周鹤翔
Owner BEIJING NORMAL UNIVERSITY
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