Facile radiolabeling optimization process via design of experiments and an intelligent optimization algorithm: Application for omeprazole radioiodination

Abstract

The major uses of radiopharmaceuticals (RP) in clinical areas are diagnosis and/or therapy. The present study aimed to utilize the application of fractional factorial design analysis (FFDA) coupled with particle swarm optimization algorithm (PSO) to assess the optimization of RP production process. In this regard, omeprazole (OMP), which is gastric parietal cell proton pump inhibitor (PPI), was radiolabeled with iodine‐125 (125I) isotope in order to be used as a radiotracer for stomach imaging. Different factors that affect radiolabeling process were studied. According to the proposed design, just 16 experimental runs of radiolabeling process were performed using the extremes of each factor. In addition, one run was executed at the mean point of each factor. Undesirable maximum radiolabeling yield (RY) of radioiodinated omeprazole (125I‐OMP) was deduced from application of FFDA (88.4%). Furthermore, after applying PSO with changing limits of one factor, the maximum RY of 125I‐OMP was found to be 93.78%. Moreover, the practically verification from optimum conditions, which obtained from PSO, was found to give an RY of 93.99%. Overall, the findings of this study confirmed the potential use of that hybrid design for optimization of radiolabeling processes.

Novel radioiodinated desvenlafaxine‐loaded lipid nanocapsule for brain delivery

“…The radiochemical yield is unaffected by the further increase in reaction time beyond 180 min. [ 29 ]…”

Radiolabeling chemistry with heavy halogens iodine and astatine

“…Regioselectivity of substitution reaction is governed by inductive and resonance effects of substituents, the most activating (electron donating) onespromoting ortho and para positions. Examples of radiopharmaceuticals of interest obtained by this approach include the 125 I-labeled Omeprazol for stomach imaging (Farrag et al, 2019) whereas direct radioastatination proved less efficient when studying the 211 At-labeling of methylene blue for melanoma treatment that required elevated temperature >100°C (Norseev, 1998) or in the context of protein labeling (vide infra). Even if radioiodination reaction is fast, simple to perform and often results in high RCYs and A m , polyiodination and formation of positional isomers are non-negligible limits.…”