Radiolabeling and Quality Control Studies of Cefdinir Solid Dispersions with Polyvinyl Alcoholas Possible Infection and Inflammation Imaging Agent


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Ekinci M., Öztürk A. A., İlem Özdemir D.

EUFEPS Annual Meeting 2023, Lisbon, Portugal, 31 May - 02 June 2023, pp.179

  • Publication Type: Conference Paper / Summary Text
  • City: Lisbon
  • Country: Portugal
  • Page Numbers: pp.179
  • Anadolu University Affiliated: Yes

Abstract

Easy and early detection of infection and inflammation is essential for early and effective treatment. In this study, solid dispersions (SDs) of cefdinir (CEF) using polyvinyl alcohol (PVA) were prepared and radiolabeled with [99mTc]NaTcOto develop potential radiotracers for detection of infection/inflammation. Radiolabeling efficiency and in vitro stability of [99mTc]Tc-CEF-SDs were determined using radioactive thin layer chromatography (RTLC). For the preparation of SDs, CEF (0.5 g) was suspended in methanol (50 mL). While mixing with magnetic stirrer, CEF suspension was added to polymer solution (0.5 g PVA in 50 mL distilled water) and the mixture was sonicated using probe sonicator (75% amplitude, 8 min). CEF-SDs were then refrigerated at -80°C and lyophilized to obtain a fine powder. [1] Then, the SDs solutions (1 mL) were radiolabeled with [99mTc]NaTcOusing stannous chloride (0.5 mg.mL-1 in distilled water) as the reducing agent. [2] Radiolabeling was performed with freshly eluted [99mTc]NaTcO(37 MBq) in 0.9% sodium chloride solution (SF, 0.1 mL). The mixture was shaken for 30 s and then incubated for 15 min at 25°C. Next, the RTLC method was used to determine the radiolabeling efficiency. Aliquots (10 μL) of the radio-mixtures were applied to the origin of the ITLC-SG plates and dried at room temperature. The plates were then developed using appropriate solvent systems. Acetone was used to determine free- [99mTc]NaTcO4, whereas SF was used to determine the radiocolloid. After development, the plates were dried and the radioactivity distribution was determined using a TLC scanner. Based on the obtained results, high radiolabeling efficiency was achieved for [99mTc]Tc-CEF-SDs (92%). To test the stability of [99mTc]Tc-CEF-SDs in SF, 0.1 mL of [99mTc]Tc-CEF-SDs was added to 0.4 mL of SF. The mixture was then incubated at 25°C for 6 h. The radiolabeling efficiency remained stable, with some insignificant changes for the [99mTc]Tc-CEF-SDs at 25°C for 6 h. In conclusion, the newly developed radiotracer ([99mTc]Tc-CEF-SDs) may be useful for further studies that are in progress to evaluate the bacterial binding capacity and biodistribution of the complex in experimental animals for detection of infection/inflammation.