Design of Tc-99(m) radiolabeled gemcitabine polymeric nanoparticles as drug delivery system and in vivo evaluation

Abstract

The main objective of this study is to create a multifunctional drug carrier system as a prototype product. For this purpose, Gemcitabine that used as an anticancer agent for several kinds of tumour therapy, and technetium(I)-tricarbonyl core, [Tc-99m(CO)(3)](+), was incorporated to the polymeric structure. In the current study PLA-PEG-COOH (polylactic acid-polyethylene glycol-carboxyl) copolymer was synthesized and the structure analysis was performed by FT-IR and H-1 NMR. The surface charge, size and morphology of the polymeric nanoparticles was evaluated by Zeta Potential (ZP) analysis, Dynamic Light Scattering (DLS) and Scanning Electron Microscopy (SEM) methods. Gemcitabine loaded polymeric nanoparticles were radiolabeled with [Tc-99m(CO)(3)(H2O)(3)](+) and quality controls were performed by thin layer radiochromatograpy (TLRC) and high performance liquid radiochmmatograpy (HPLRC). PLA-PEG-GEM complex was labeled with [Tc-99m(CO)(3)](+) in high radiochemical yield and purity. The radiolabeled complex is stable during the study period in saline solution. The biological activity of this radiolabeled system was evaluated performing biodistribution and gamma camera imaging on Wistar Albino rats which exhibited higher uptake in the lung and liver at all selected time points.