Brain tumor magnetic resonance contrast agent and its preparation method

A technology for magnetic resonance contrast agents and brain tumors, which can be used in pharmaceutical formulations, preparations for in vivo tests, emulsion delivery, etc. It can solve the problems of poor hepatic cholangiography, low tissue specificity, and short imaging time. Strong contrast effect, high specificity, and low toxic and side effects

Inactive Publication Date: 2012-11-21
XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Gadolinium-based contrast agents effectively improve the diagnostic level of magnetic resonance imaging MRI, but Gd-DTPA has low relaxation rate, non-biocompatibility, low tissue specificity, high osmotic pressure, short imaging time, and fast diffusion. Low selectivity, poor effect on hepatic cholangiography, toxicity is related to the metabolic process of free gadolinium in the body, causing nephrogenic systemic fibrosis

Method used

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  • Brain tumor magnetic resonance contrast agent and its preparation method
  • Brain tumor magnetic resonance contrast agent and its preparation method
  • Brain tumor magnetic resonance contrast agent and its preparation method

Examples

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Embodiment 1

[0046] Embodiment 1: Preparation of a brain tumor magnetic resonance contrast agent, which is a conjugate of transferrin and superparamagnetic iron oxide nanoparticles, i.e. Transferrin-SPIO, with a particle size of about 14 nanometers, comprising the following steps:

[0047] (1) Prepare activated superparamagnetic iron oxide nanoparticle suspension: get superparamagnetic iron oxide nanoparticle, disperse in 1mol / L sodium acetate buffer solution of pH=5.0, add EDC and NHS (final concentration is respectively 5mM and 12.5mM), shake for 15 minutes, remove unreacted EDC and NHS with a magnet, then add 0.1mol / L PBS buffer solution with pH=7.4 to redisperse superparamagnetic iron oxide nanoparticles at a ratio of 2mg: 200ul to obtain activated Suspension of superparamagnetic iron oxide nanoparticles.

[0048] (2) Preparation of transferrin solution: Dissolve transferrin in 0.1 mol / LPBS buffer solution with pH=7.4 at a ratio of 0.2 mg:200 ul.

[0049] (3) Add the prepared transfer...

Embodiment 2

[0052] Embodiment 2: Transmission electron microscopy (TEM) comparison of superparamagnetic iron oxide nanoparticles before and after coupling transferrin

[0053] Getting the concentration prepared in Example 1 is that the superparamagnetic iron oxide nanoparticles coupled with transferrin of 10 mg / mL is detected by transmission electron microscope, and the transmission electron microscope (TEM) of the superparamagnetic iron oxide nanoparticles ( TEM) photos, see image 3 . The transmission electron microscope (TEM) photo of superparamagnetic iron oxide nanoparticles before coupling transferrin is shown in figure 2 . figure 2 It shows that the particle diameter of superparamagnetic iron oxide nanoparticles is 9 nanometers; image 3 The particle size of the superparamagnetic iron oxide nanoparticles coupled with transferrin was shown to be 14 nm.

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Abstract

The invention provides a brain tumor magnetic resonance contrast agent. The contrast agent is transferrin coupled super-paramagnetic iron oxide nanoparticles and contains a physiologically acceptable diluent, wherein the diluent can be PBS (phosphate buffer solution) or normal saline; the weight/volume application ratio of the transferrin coupled super-paramagnetic iron oxide nanoparticles to the diluent is 10-20mg:1mL; the super-paramagnetic iron oxide nanoparticles can be super-paramagnetic ferric oxide nanoparticles or super-paramagnetic ferriferrous oxide nanoparticles; and the particle sizes of the super-paramagnetic iron oxide nanoparticles are 10-20nm. The contrast agent utilizes the high affinity between the transferrin and transferrin acceptors expressed on surfaces of cells to realize the targeting developing, and has the characteristics of high specificity, good selectivity, strong contrast effect, low toxic side effect, enough tissue concentration for the in-vivo imaging, and the like.

Description

technical field [0001] The invention belongs to the technical field of medical detection reagents, in particular to a brain tumor-specific contrast agent used for MRI (magnetic resonance imaging) contrast enhancement and a preparation method thereof. Background technique [0002] Brain tumor is a common intracranial disease that seriously endangers human health, with high disability and mortality and poor curative effect. In the past 20 years, the clinical application of magnetic resonance has greatly improved and advanced the imaging diagnostic technology of the central nervous system. It can safely and effectively present the structure and function of human tissues and organs. It has been used as a routine inspection method in clinical diagnosis. be applied. More than 30% of MRI examination cases require the use of contrast agents to improve the imaging contrast between normal tissues and lesions, thereby improving the resolution of soft tissue images and making MRI more ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/14A61K49/18
Inventor 徐海波杨祥良蒋玮丽谢辉姜冬玲刘芳尚亚雷朱艳红赵彦斌石浩军李欢尹明媛
Owner XIEHE HOSPITAL ATTACHED TO TONGJI MEDICAL COLLEGE HUAZHONG SCI & TECH UNIV
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