Preparation of99mTc-EDTA-MN and Its Bioimaging in Mouse
10.3779/j.issn.1009-3419.2015.07.06
- VernacularTitle:99mTc-EDTA-MN的制备及其在荷瘤裸鼠显像中的初步评价
- Author:
QI YONGSHUAI
1
;
LI GUIPING
;
CHI XIAOHUA
;
DU LI
;
HUANG KAI
;
ZHANG HUI
;
HUANG BAODAN
Author Information
1. 南方医科大学南方医院核医学科
- Keywords:
Lung neoplasms;
Hypoxia imaging agent;
Ethylenediaminetetraacetic Acid-metronidazole;
Tadio-chemical purity
- From:
Chinese Journal of Lung Cancer
2015;(7):422-426
- CountryChina
- Language:Chinese
-
Abstract:
Background and objective Hypoxia is an important biological characteristics of solid tumor, it is not sensitive to radiotherapy and chemotherapy for which is the presence of hypoxic cell, thus increasing their resistance to con-ventional radiotherapy and chemotherapy, therefore, the detection of hypoxia degree of tumor tissue is of great signiifcance. hTe hypoxia imaging of nuclear medicine can relfect the degree of tissue hypoxia, which can selectively retained on the hypoxic cells or tissues, including nitroimidazole and non nitroimidazole; the nitroimidazole is widely and deeply researched as hypoxic celles developer in China and abroad at present. hTe research about application of radionuclide labelled technique has clini-cal application value to develop the hypoxia imaging agent EDTA-MN complexes which was labeled. To study the feasibility of99mTc by direct labeling method, the radiochemical properties evaluation of99mTc-EDTA-MN, and observe the distribution characteristics of99mTc radiolabeled EDTA-MN in the xenogratf lung cancer nude mice bearing non-small cell lung cancer cell (A549), and provide experimental evidence for its further research and application.MethodshTe radiolabeling of EDTA-MN with99mTc was performed with direct labeling method, respectively, on the reaction dosage (10 mg, 5 mg, 2 mg), stannous chlo-ride dosage (8 mg/mL, 4 mg/mL, 2 mg/mL), mark system pH (2, 4, 5, 6) one by one test, using orthogonal design analysis, to ifnd the optimal labeling conditions. Labelling rate, radiochemical purity, lipid-water partition coeffcient and in vitro stability in normal saline (NS) were determined by TLC and HPLC, and the preliminary study on the distribution of99mTc-EDTA-MN in nude mice.Results hTe labeling rate of99mTc-EDTA-MN with the best labeling conditions was (84.11±2.83)%, and the ra-diochemical purity was higher than 90% by HPLC puriifcation, without any notable decomposition at room temperature over a period of 12 h. hTe partition coeffcient was lgP=-3.05, indicated that this complex was hydrophilic. At 3 h post-injection, the imaging of99mTc-EDTA-MN in nude mice bearing non-small cell lung cancer cell showed that more radioactive gathered in bladder at0.5 h, the transplanted tumor was clearly imaged at 1 h post-injection, during whole imaging radioactive in other tissues and organs was low. hTe radioactivity of tumor uptake by using of ROI technology were (88.14±11.59), (123.17±9.06), (98.08±14.40) and (79.87±10.57) at 0.5, 1, 2, 3 h post-injection, and the ratio of T/NT of tumor and liver area were (1.95± 0.19), (3.58±0.78), (3.95±0.39) and (5.01±0.28), respectively.99mTc-EDTA-MN could be quickly cleared from the blood in mice primarily through the kidneys, and the radioactivity in other tissues and organs remained low.Conclusion99mTc-EDTA-MN can be easily prepared and labeled compound with high labeling rate and stability, it appears to be suitable for further experiments requirementin vivo andin vitroapplication.
