Optimizing the radiolabeling of block copolymer micelles using 89Zr

Bachelor thesis (2022)

Authors

S. Vonk Applied Sciences

Contributors

A.G. Denkova RST/Applied Radiation & Isotopes - AS (mentor)
E.J. van den Heuvel RST/Technici Pool - AS (mentor)
Faculty
Applied Sciences, Applied Sciences
Copyright: © 2022 Stefan Vonk
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Published Date

07-07-2022

Language

English

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Faculty

Applied Sciences

Abstract

Polymeric micelles are increasingly used in chemotherapy. To get a greater understanding of the behaviour of these micelles is important. Nuclear imaging, such as SPECT and PET can provide relevant information about the behaviour of the micelles. However, to use these techniques, the micelles must be radiolabelled. In this thesis a chelator free method will be described to radiolabel micelles. The goal of this thesis is to radiolabel block copolymers with Zr-89. For this purpose series of experiments were carried out. In these experiments three different concentrations ZrCl4 are applied, C1 = 0.04mM, C2 = 0.07mM and C3 = 1mM. These experiments are conducted for two different types of polymer micelles, PCL-PEO 2800-2000 and PLA-PEO 10500-5000. With these polymers, micelles are prepared, which are used for the radiolabeling process. The fractions obtained by the SEC (size exclusion chromatography) were analysed and the data was processed. At the first concentration C1 = 0.04mM, PCL-PEO 2800-2000 had an efficiency of 37,65 ± 2,48 %. PLA-PEO 10500-5000 gave a radiolabeling efficiency of 28,27 ± 1,23 %. The second concentration, C2 = 0.07mM, showed a decrease in radiolabeling efficiency. For the PCL-PEO-2800-2000 polymeric micelles a radiolabeling efficiency of 23,30 ± 13,94 % was found and for the PLA-PEO 10500-5000 micelles an efficiency of 19,76 ± 1,70 was found. Lastly at the third concentration, C3 = 1mM, for PCL-PEO 2800-2000 the radiolabeling efficiency was found to be 0,88 ± 0,07 %. The PLA-PEO 10500-5000 micelles gave back 2,91 ± 1,68 % as radiolabeling efficiency. A stablity test was performed at C1 = 0.04mM. The PCL-PEO 2800-2000 polymeric micelles had a retention ratio of 37,57 ± 4,35 %. The PLA-PEO 10500-5000 performed better, 69,03 ± 1,27 % of the zirconium was still found to be in the micelles after being challenged by diethylenetriaminepentaacetic acid, or in short, DTPA. A stability test was also performed at C3 = 1mM, but results were found that are not usable. This experiment should be done again in future research.