5 years ago

Radiolabeling, quality control, and biological characterization of 177Lu-labeled kanamycin

Radiolabeling, quality control, and biological characterization of 177Lu-labeled kanamycin
Saira Hina, Muhammad Razeen Ahmad, Tanveer Hussain Bokhari, Tania Jabbar, Muhammad Sohaib, Muhammad Usman Akbar, Sajid Mehmood, Samina Roohi, Muhammad Khalid
Kanamycin is an antibiotic, isolated from Streptomyces kanamyceticus, which is used to treat serious bacterial infections. The fact that the present radioligand 99mTc-kanamycin used for diagnosis is short-lived, raised a need to label and study kanamycin with one of the most important beta (β) radiation emitting isotope 177Lu. Labeling yield of 177Lu-kanamycin was confirmed by different chromatography techniques such as paper chromatography, TLC, HPLC. Several experiments were performed to optimize labeling with changing reaction conditions such as pH, temperature, amount of ligand, and reaction time. In vitro stability analysis was performed incubation with human serum. Electrophoresis analysis was also conducted to determine the charge on 177Lu-kanamycin. The biodistribution and scintigraphy were performed in normal mice and rabbit, respectively, at different time intervals of postinjection. 177Lu-kanamycin was prepared with very high yield (~100%), with excellent stability in vivo and in vitro (>99% 6 hr postprep.), at pH 7. Maximum labeling was achieved at less reaction time (15 min), with maximum conjugation of the ligand (12.5 mg) with 177Lu. Electrophoresis analysis showed net neutral charge. The radioligand showed rapid clearance from body in biodistribution and scintigraphy studies. The preparation 177Lu-kanamycin could be used as a radio-pharmaceutical for infection imaging purpose, especially when transporting the radioligand to long-range distances. 99mTc-kanamycin, used for bacterial infection imaging, is short-lived and cannot be transported over long distances. To resolve this, kanamycin was labeled with lutetium-177, a long-lived isotope that emits β- and γ-radiation. Radiolabeling of 177Lu-kanamycin was optimized. 177Lu-kanamycin was prepared with a very high yield (~100%) and showed excellent stability in vitro. Biodistribution and scintigraphy studies in mice and rabbit showed rapid clearance from body, suggesting that 177Lu-kanamycin could be used for medical imaging.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1111/cbdd.12960

You might also like
Discover & Discuss Important Research

Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.