Preparation method of hepatocarcinoma target CT (Computed Tomography) contrast medium based on Au DENPs-LA (Dendrimer-entrapped Gold Nanoparticles-Lactobionic acid)

A contrast agent, LA-PEG-COOH technology, applied in X-ray contrast agent preparation, freeze-dried delivery, powder delivery, etc., can solve the problem of not finding liver cancer-targeted CT contrast agents

Inactive Publication Date: 2013-07-24
DONGHUA UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] A search of domestic and foreign literature and patents on the use of gold nanoparticles for CT imaging found that: before the completion of the present invention, no liver cancer based on gold nanoparticles coated with lactobionic acid modified fifth-generation polyamide-amine dendrimers has been found. Report on the preparation of targeted CT contrast agent and its performance in CT contrast

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  • Preparation method of hepatocarcinoma target CT (Computed Tomography) contrast medium based on Au DENPs-LA (Dendrimer-entrapped Gold Nanoparticles-Lactobionic acid)
  • Preparation method of hepatocarcinoma target CT (Computed Tomography) contrast medium based on Au DENPs-LA (Dendrimer-entrapped Gold Nanoparticles-Lactobionic acid)
  • Preparation method of hepatocarcinoma target CT (Computed Tomography) contrast medium based on Au DENPs-LA (Dendrimer-entrapped Gold Nanoparticles-Lactobionic acid)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Take 56.45 mg of lactobionic acid (LA-COOH), dissolve it in 6 mL of disodium hydrogen phosphate-sodium dihydrogen phosphate buffer solution (pH6.0, 0.02M), and shake it magnetically to fully dissolve it evenly. Add 0.763 mL (39.59 mg / mL) of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) and 0.829 mL (21.87 mg / mL) of N-hydroxysuccinimide (NHS) mg / mL), stirred for 3h. Take polyethylene glycol (two ends are amino and carboxyl, NH 2 -PEG-COOH, Mw2000) 175.48 mg, dissolved in 8 mL of disodium hydrogen phosphate-sodium dihydrogen phosphate buffer (pH6.0, 0.02M). Subsequently, the activated lactobionic acid solution was added to the polyethylene glycol solution, and the reaction was stirred for 3d. Afterwards, the resulting solution was dialyzed against distilled water (6 times, 2 L / time), and then freeze-dried to obtain polyethylene glycol-lactobionic acid (LA-PEG-COOH), which was stored at -20°C.

[0058] Take 6.52 mg of fluorescein isothiocyanate (FITC...

Embodiment 2

[0061] Weigh 205.85 mg of LA-PEG-COOH prepared in Example 1, and dissolve it in 8 mL of distilled water. During magnetic stirring, EDC0.858mL (93.24mg / mL) and NHS0.838mL (57.33mg / mL) were added, and the reaction was stirred for 3h.

[0062] Get the G5.NH prepared in Example 1 2-FI82.78mg, dissolved in 6mL distilled water. Subsequently, 9.766 mL of the activated LA-PEG-COOH solution was added, and the reaction was performed with magnetic stirring for 3 days. After the reaction, the resulting solution was dialyzed against distilled water (6 times, 2 L / time). Then freeze-dried to obtain lactobionic acid-modified dendrimers (G5.NH 2 -FI-PEG-LA), stored at -20°C.

[0063] 1 The H NMR spectrum results show that the peak at 3.5ppm is the characteristic peak of polyethylene glycol, indicating that it has been successfully modified on the surface of dendrimers (attached figure 1 c).

Embodiment 3

[0065] Get the G5.NH prepared in Example 2 2 -FI-PEG-LA76.67mg, dissolved in 76mL of distilled water. Add 2.786mL of chloroauric acid solution (30mg / mL), and stir for 20min. Sodium borohydride solution 0.663 mL (34.72 mg / mL) was then added. The reaction was stirred for 2h.

[0066] After reacting for 2 hours, 0.126 mL of triethylamine was added and stirred for 0.5 hours. After that, 0.071 mL of acetic anhydride was added, and the reaction was stirred for 24 h. After the reaction, the reaction mixture was dialyzed with PBS buffer (3 times, 2 L / time) and distilled water (3 times, 2 L / time). Then, freeze-drying was performed to obtain lactobionic acid-modified dendrimer-wrapped gold nanoparticles (Au DENPs-LA), which were stored at -20°C.

[0067] 1 The results of the H NMR spectrum showed that the peak of acetylmethyl group (1.87ppm) appeared after the acetylation reaction, indicating that the acetylation reaction was successfully carried out (attached figure 1 d). The U...

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Abstract

The invention relates to a preparation method of a hepatocarcinoma target CT (Computed Tomography) contrast medium based on Au DENPs-LA (Dendrimer-entrapped Gold Nanoparticles-Lactobionic acid). The method comprises the following steps of: modifying a fifth generation polyamide-amine dendrimer of an amino terminal with fluorescein, connecting lactobionic acid with the dendrimer through polyethylene glycol, taking the modified dendrimer as a template, preparing gold nanoparticles by reduction of sodium borohydride, performing acetylation treatment on left amino on the surface of the dendrimer wholly, dialyzing a reacted solution, performing freeze drying treatment, obtaining a finished hepatocarcinoma target CT contrast medium, and evaluating the external CT performance and internal CT performance of the contrast medium. The method is simple and easy to implement; prepared Au DENPs-LA has good stability, aqueous solution dispersity and biocompatibility, shows a good external hepatocarcinoma cell target effect, has a specific target tumour CT effect, and has a potential target CT application prospect.

Description

technical field [0001] The invention belongs to the field of preparation of contrast agents, in particular to a preparation method of liver cancer-targeted CT contrast agents based on Au DENPs-LA. Background technique [0002] Cancer (also known as malignant tumor in medical terms) has become the number one killer affecting human health due to its high lethality and refractory nature. This is mainly because cancer cells have the characteristics of local invasion and distant metastasis, which are difficult to diagnose and find in the early stage, and difficult to treat and control in the late stage. At present, researchers from many countries are working on the early diagnosis and treatment of cancer. [0003] CT technology has become one of the most widely used molecular imaging methods because of its excellent spatial and density resolution, and is widely used in clinical practice. At this stage, the use of CT technology in the diagnosis of cancer is very limited. At pre...

Claims

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Application Information

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IPC IPC(8): A61K49/04A61K9/19
Inventor 史向阳刘辉张贵祥王悍许艳红
Owner DONGHUA UNIV
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