Radiolabeling of Preformed Niosomes With [ 99M Tc]: In Vitro Stability, Biodistribution, and in Vivo Performance Publisher Pubmed



Almasi A¹ ; Shahhosseini S² ; Haeri A¹ ; Daha FJ³ ; Geramifar P⁴ ; Dadashzadeh S^{1, 5} Show Affiliations
Source: AAPS PharmSciTech Published:2018

Abstract

Nanocarriers radiolabeled with [ 99m Tc] can be used for diagnostic imaging and radionuclide therapy, as well as tracking their pharmacokinetic and biodistribution characteristics. Due to the advantages of niosomes as an ideal drug delivery system, in this study, the radiolabeling procedure of niosomes by [ 99m Tc]-HMPAO complexes was investigated and optimized. Glutathione (GSH)-loaded niosomes were prepared using a thin-film hydration method. To label the niosomes with [ 99m Tc], the preformed GSH-loaded niosomes were incubated with the [ 99m Tc]-HMPAO complex and were characterized for particle size, size distribution, zeta potential, morphology, and radiolabeling efficiency (RE). The effects of GSH concentration, incubation time, incubation temperature, and niosomal composition on RE were investigated. The biodistribution profile and in vivo SPECT/CT imaging of the niosomes and free [ 99m Tc]-HMPAO were also studied. Based on the results, all vesicles had nano-sized structure (160–235 nm) and negative surface charge. Among the different experimental conditions that were tested, including various incubation times, incubation temperatures, and GSH concentrations, the optimum condition that resulted in a RE of 92% was 200-mM GSH and 15-min incubation at 40°C. The in vitro release study in plasma showed that about 20% of radioactivity was released after 24 h, indicating an acceptable radiolabeling stability in plasma. The biodistribution of niosomes was clearly different from the free radiolabel. Niosomes carrying radionuclide were successfully used for tracking the in vivo disposition of these carriers and SPECT/CT imaging in rats. Furthermore, biodistribution studies in tumor-bearing mice revealed higher tumor accumulation of the niosomal formulation as compared with [ 99m Tc]-HMPAO. © 2018, American Association of Pharmaceutical Scientists.