Preparation, radiolabeling and cell culture studies of chitosan coated PLGA nanoparticles as a potential cancer diagnostic agent

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

Journal of Research in Pharmacy, vol.26, no.6, pp.1636-1645, 2022 (Scopus) identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 6
  • Publication Date: 2022
  • Doi Number: 10.29228/jrp.254
  • Journal Name: Journal of Research in Pharmacy
  • Journal Indexes: Scopus, TR DİZİN (ULAKBİM)
  • Page Numbers: pp.1636-1645
  • Keywords: cell culture, Chitosan, diagnostic nanosystem, nanoparticle, PLGA, radiolabeling, technetium-99m
  • Anadolu University Affiliated: Yes


Using the nanoprecipitation process, chitosan coated poly lactic-co-glycolic acid (PLGA) based polymeric nanoparticle formulations of two molecular weights were developed as a possible cancer cell diagnostic agent. Photon correlation spectroscopy was used to measure the particle size, distribution [polydispersity index (PDI)], and zeta potential values of developed nanoparticle formulations. The F1 [low molecular weight PLGA (Resomer® RG 503 H)] and F2 [high molecular weight PLGA (Resomer® RG 504 H)] formulations were then directly labeled with Technetium-99m ([99mTc]Tc) using stannous salts (chloride) as a reducing agent. The radiochemical purity (RP) and in vitro stability in different mediums of the formulations were assessed using ascending radioactive thin layer chromatography (RTLC) method. The cell incorporation of [99mTc]Tc labeled F1 and F2 formulations, as well as Reduced/Hydrolized [99mTc]NaTcO4 (R/H-[99mTc]NaTcO4) in the MCF-7 (breast cancer cell line) cells, was then assessed. The nanoparticles had a middle size of 408.9±3.626 nm to 421.3±7.205 nm, a PDI value of 0.310±0.055 to 0.330±0.066, and a positive charge of +70.5±1.4 mV to +75.5±3.8 mV, according to the characterization results. F1 and F2 formulations were effectively radiolabeled with [99mTc]Tc, and their RP was found to be over 98% in both cases. When compared to [99mTc]Tc-F1 (45.091±2.254%) and R/H-[99mTc]NaTcO4 (8.527±0.426%), the incorporation percentages of [99mTc]Tc-F2 (70.756±3.537%) were shown to be higher in cancer cell lines (breast cancer cells, MCF-7). According to this research, radiolabeled chitosan coated PLGA nanoparticles ([99mTc]Tc-F2) could be suggested as promising cancer detection formulations. However, further investigations, such as biodistribution studies, should be performed.