Journal article
Preparation and pharmacological evaluation of a new radiopharmaceutical, technetium-99m-5-fluorouracil, for tumor scintigraphy
Hellenic journal of nuclear medicine, Vol.11(2), pp.91-95
05/01/2008
PMID: 18815662
Abstract
5-fluorouracil (5-FU) has been used for cancer chemotherapy since more than four decades. There are reports of use of F-18 and F-19 analogues of 5-FU for tumor studies using positron emission tomography (PET) and nuclear magnetic imaging (NMR), respectively. However, study pertaining to its use in g-scintigraphy is still lacking. In the present study, we have optimized the methodology to radiolabel it with technetium-99m (Tc-99m) efficiently and evaluated its physicochemical and biological properties. Methods: 5-FU was radiolabeled with Tc-99m and evaluated for physicochemical properties. Blood kinetics were studied in rabbits and biodistribution was carried out in normal as well as tumor bearing mice. In vivo and in vitro tumor uptake of the radiocomplex was evaluated in Ehrlich Ascites Tumor (EAT) bearing mice and human breast cancer cell line (MDA-MB-468). Results: The resultant radiopharmaceutical (Tc-99m-5-FU) has been found to be stable up to 24 h in both in vitro normal and physiological conditions. The blood clearance of the Tc-99m-5-FU showed a bi-phasic pattern. High extraction of Tc-99m-S-FU by the liver (36.41 +/- 2.79 % of injected dose/g tissue) has been observed in mice, along with time dependent increase in the solid tumor to muscle ratio (2: 1) measured at 4 h. Incubation of the radiocomplex with human breast cancer cells lines also showed time dependent increase in the uptake of the tracer. Conclusion: It can be concluded that the Tc-99m-5-FU possesses selectivity towards solid tumor tissue.
Details
- Title: Subtitle
- Preparation and pharmacological evaluation of a new radiopharmaceutical, technetium-99m-5-fluorouracil, for tumor scintigraphy
- Creators
- Santosh Kumar - Birla Inst Technol, Dept Pharmaceut Sci, Ranchi 835215, Bihar, IndiaAnil Kumar Mishra - College Station Medical CenterBhupender S. Chhikara - College Station Medical CenterKrishna Chuttani - College Station Medical CenterRakesh Kumar Sharma - Def Res Lab, Tejpur 784001, Assam, India
- Resource Type
- Journal article
- Publication Details
- Hellenic journal of nuclear medicine, Vol.11(2), pp.91-95
- Publisher
- Hellenic Soc Nuclear Medicine
- PMID
- 18815662
- ISSN
- 1790-5427
- eISSN
- 1790-5427
- Number of pages
- 5
- Language
- English
- Date published
- 05/01/2008
- Academic Unit
- Cardiovascular Medicine; Internal Medicine
- Record Identifier
- 9984359591002771
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