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[99mTc]Technetium-Labeled Niosomes: Radiolabeling, Quality Control, and <i>In Vitro</i> Evaluation

Ekinci, Meliha; Caliskan, Emine Esin; Cakar, Burak; Ilem-Ozdemir, Derya; Uyanikgil, Yigit; Uyanikgil, Emel Oyku Cetin


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    "creators": [
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        "affiliation": "Ege Univ, Fac Pharm, Dept Radiopharm, TR-35040 Izmir, Turkiye", 
        "name": "Ekinci, Meliha"
      }, 
      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Technol, Dept Biopharmaceut & Pharmacokinet, TR-35100 Izmir, Turkiye", 
        "name": "Caliskan, Emine Esin"
      }, 
      {
        "affiliation": "Ege Univ, Fac Med, Dept Histol & Embryol, TR-35040 Izmir, Turkiye", 
        "name": "Cakar, Burak"
      }, 
      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Radiopharm, TR-35040 Izmir, Turkiye", 
        "name": "Ilem-Ozdemir, Derya"
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      {
        "affiliation": "Ege Univ, Hlth Sci Inst, Fac Med, Cell & Tissue Res & Applicat Ctr,Dept Hist & Embr, TR-35040 Izmir, Turkiye", 
        "name": "Uyanikgil, Yigit"
      }, 
      {
        "affiliation": "Ege Univ, Fac Pharm, Dept Pharmaceut Technol, Dept Biopharmaceut & Pharmacokinet, TR-35100 Izmir, Turkiye", 
        "name": "Uyanikgil, Emel Oyku Cetin"
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    "description": "<p>The aim of this research was to develop technetium-99m ([99mTc]Tc)-radiolabeled niosomes and evaluate the cancer cell incorporation capacity of radiolabeled niosomes. For this purpose, niosome formulations were developed by film hydration method, and prepared niosomes were characterized to particle size, polydispersity index (PdI), zeta-potential value, and image profile. Then, niosomes were radiolabeled with [99mTc]Tc using stannous salts (chloride) as a reducing agent. The radiochemical purity (RP) and stability in different mediums of the niosomes were assessed by ascending radioactive thin-layer chromatography (RTLC) and radioactive ultrahigh-performance liquid chromatography (R-UPLC) methods. Also, the partition coefficient value of radio-labeled niosomes was determined. The cell incorporation of [99mTc]Tc-labeled niosome formulations, as well as reduced/hydrolyzed (R/H)-[99mTc]NaTcO4 in the HT-29 (human colorectal adenocarcinoma) cells, was then assessed. According to the obtained results, the spherical niosomes had a particle size of 130.5 +/- 1.364 nm, a PdI value of 0.250 +/- 0.023, and a negative charge of -35. 4 +/- 1.06 mV. The niosome formulations were effectively radiolabeled with [99mTc]Tc using 500 mu g mL-1 stannous chloride for 15 min, and RP was found to be over 95%. [99mTc]Tc-niosomes showed good in vitro stability in every system for up to 6 h. The log P value of radiolabeled niosomes was found as -0.66 +/- 0.02. Compared to R/H-[99mTc]NaTcO4 (34.18 +/- 1.56%), the incorporation percentages of [99mTc]Tc-niosomes (88.45 +/- 2.54%) were shown to be higher in cancer cells. In conclusion, the newly developed [99mTc]Tc-niosomes showed good prototype for potential use in nuclear medicine imaging in the near future. However, further investigations, such as drug encapsulation and biodistribution studies, should be performed, and our studies are continuing.</p>", 
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    "journal": {
      "pages": "10", 
      "title": "ACS OMEGA"
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    "license": {
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    "publication_date": "2023-01-01", 
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    "title": "[99mTc]Technetium-Labeled Niosomes: Radiolabeling, Quality Control, and <i>In Vitro</i> Evaluation"
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