Development of Tc-99m radiolabeling PLGA parameters nanoparticles: Preparation, characterization and evaluation of radiolabeling parameters

Year 2025, Volume: 29 Issue: 4, 1753 - 1759, 05.07.2025

Elif Tugce Sarcan , Hümeyra Battal , Mine Silindir-günay , Suna Erdoğan

https://doi.org/10.12991/jrespharm.1734690

Abstract

Radiolabeled polymeric NPs are widely used drug delivery systems in cancer therapy and imaging due to their easy and rapid formation. These systems provide several advantages for imaging and therapy of many diseases and cancers, such as increased sensitivity, better image quality, etc. In this study, Tc-99m radiolabeled PLGA nanoparticles were prepared in different conditions and these conditions were investigated. The amount of reducing agent, incubation temperature and time, and pH were investigated to obtain the 99mTc-PLGA nanoparticles with higher RCP (%). NPs were formed well with the nanoprecipitation method between 180-200 nm. Then, the optimum formulation was obtained with 50 µl SnCl2 at pH 7 and 25 ºC conditions for 30 minutes of incubation time. This formulation was found stable at 25 ºC for 12 hours while showing 3 hours of stability at 37 ºC. The data proved that PLGA NPs can be radiolabeled with Tc-99m at high efficiency and showed relatively high radiolabeling stability.

Keywords

Technetium-99m , PLGA nanoparticles , radiolabelling , radiopharmaceuticals

References

• [1] Varani M, Campagna G, Bentivoglio V, Serafinelli M, Martini ML, Galli F, Signore A. Synthesis and biodistribution of 99mTc-Labeled PLGA nanoparticles by microfluidic technique. Pharmaceutics. 2021;13(11):1769. https://doi.org/10.3390/pharmaceutics13111769
• [2] Chiu HI, Samad NA, Fang L, Lim V. Cytotoxicity of targeted PLGA nanoparticles: A systematic review. RSC Adv. 2021; 11(16): 9433. https://doi.org/10.1039/D1RA00074H
• [3] Schoubben A, Ricci M, Giovagnoli S. Meeting the unmet: From traditional to cutting-edge techniques for poly lactide and poly lactide-co-glycolide microparticle manufacturing. J Pharm Investig. 2019; 49: 381-404. https://doi.org/10.1007/s40005-019-00446-y
• [4] Prabhu R, Patravale V, Joshi MD. Polymeric nanoparticles for targeted treatment in oncology: Current insights. Int J Nanomed. 2015; 10: 1001-1018. https://doi.org/10.2147/IJN.S56932
• [5] Zhang X, Yan R, Wei Z, Yang D, Hu Z, Zhang Y, Huang X, Huang H, Wang W. Folate decorated multifunctional biodegradable nanoparticles for gastric carcinoma active targeting theranostics. Int J Nanomed. 2022; 12: 2493-2502. https://doi.org/10.2147/IJN.S348380 [6] Hong H, Zhang Y, Sun J, Cai W. Molecular imaging and therapy of cancer with radiolabelled nanoparticles. Nano Today. 2009; 4(5): 399-413. https://doi.org/10.1016/j.nantod.2009.07.001
• [7] Loudos G, Kagadis GC, Psimadas D. Current status and future perspectives of in vivo small animal imaging using radiolabelled nanoparticles. Eur J Radiol. 2011; 78(2): 287-295. https://doi.org/10.1016/j.ejrad.2010.06.025
• [8] Chakravarty R, Goel S, Dash A, Cai W. Radiolabeled inorganic nanoparticles for positron emission tomography imaging of cancer: an overview. Q J Nucl Med Mol Imaging. 2017; 61(2): 181-204. https://doi.org/10.23736/S1824 4785.17.02969-7
• [9] after Snehalatha M, Venugopal K, Saha RN. Etoposide loaded PLGA and PCL nanoparticles II: Biodistribution and pharmacokinetics radiolabelling 99mTc-labeled with Tc-99m. Drug Deliv. 2008; 15(5): 277-287. https://doi.org/10.1080/10717540802006500
• [10] Arulsudar N, Subramanian N, Mishra P, Sharma RK, Murthy RS. Preparation, characterization and biodistribution of liposome encapsulated cyclosporine. J Drug Target. 2003; 11(3): 187-196. https://doi.org/10.1080/10611860310001615415
• [11] Oda CMR, Fernandes RS, de Araujo Lopes SC, de Oliveria MC, Cardoso VN, Santos DM, de Castro Pimenta AM, Malachias A, Paniago R, Townsdend DM, Colletti PM, Rubello Di Alves RJ, de Barros ALB, Leite EA. Synthesis, characterization and radiolabelling of polymeric nano-micelles as a platform for tumor delivering. Biomed Pharmacother. 2017; 89: 268-275. https://doi.org/10.1016/j.biopha.2017.01.144
• [12] He Z, Zhang X, Huang J, Wu Y, Huang X, Chen J, Xia J, Jiang, H, Ma J, Wu J. Immune activity and biodistribution of polypeptide K237 and folic acid conjugated amphiphilic PEG-PLGA copolymer nanoparticles radiolabeled with Tc-99m. Oncotarget. 2016; 7(47): 76635-76646. https://doi.org/10.18632/oncotarget.12850
• [13] Sarcan ET, Silindir Gunay M, Ozer AY. Theranostic polymeric nanoparticles for NIR imaging and photodynamic therapy. Int J Pharm. 2018; 551(1-2): 329-338. https://doi.org/10.1016/j.ijpharm.2018.09.019
• [14] Halder KK, Mandal B, Debneth MC, Bera H, Ghosh LK, Gupta BK. Chloramphenicol-incorporated poly lactide-co glycolide (PLGA) nanoparticles: Formulation, characterization, technetium-99m labeling and biodistribution studies. J Drug Target. 2008; 16(4): 311-320. https://doi.org/10.1080/10611860801899300
• [15] Baishya R, Nayak DK, Kumar D, Sinha S, Gupta A, Ganguly S, Debnath MC. Ursolic acid loaded PLGA nanoparticles: In vitro and in vivo evaluation to explore tumor targeting ability on B16F10 melanoma cell lines. Pharm Res. 2016; 33(11): 2691-2703. https://doi.org/10.1007/s11095-016-1994-1
• [16] Fessi H, Puisieux F, Devissaguet JPH, Ammoury N, Benita S. Nanocapsule formation by interfacial polimer deposition following solvent displacement. Int J Pharm. 1989; 55(1): R1-R4. https://doi.org/10.1016/0378 5173(89)90281-0
• [17] Varani M, Bentivoglio V, Lauri C, Ranieri D, Signore A. Methods for Radiolabelling Nanoparticles: SPECT Use (Part 1). Biomolecules. 2022; 12(10): 1522. https://doi.org/10.3390/biom12101522
• [18] Saha GB. Quality control of radiopharmaceuticals. In: Saha GB (Ed). Fundamentals of Nuclear Pharmacy. Springer, 2018, pp. 163-183.