Radiolabeling, quality control, and biological characterization of177Lu-labeled kanamycin.
Kanamycin is an antibiotic, isolated from Streptomyces kanamyceticus, which is used to treat serious bacterial infections. The fact that the present radioligand99mTc-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 isotope177Lu. Labeling yield of177Lu-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 on177Lu-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) with177Lu. Electrophoresis analysis showed net neutral charge. The radioligand showed rapid clearance from body in biodistribution and scintigraphy studies. The preparation177Lu-kanamycin could be used as a radio-pharmaceutical for infection imaging purpose, especially when transporting the radioligand to long-range distances.
Department of Chemistry, Government College University, Faisalabad, Pakistan.|Department of Applied Chemistry and Biochemistry, Government College University, Faisalabad, Pakistan.
Muhammad Usman
http://orcid.org/0000-0001-9474-1923
MU
Akbar
Department of Chemistry, Government College University, Faisalabad, Pakistan.
Tanveer Hussain
TH
Bokhari
Isotope Production Division, Pakistan Institute of Nuclear Science and Technology, Islamabad, Pakistan.
Muhammad
M
Khalid
Department of Bioinformatics and Biotechnology, Government College University, Faisalabad, Pakistan.
Muhammad Razeen
MR
Ahmad
Isotope Production Division, Pakistan Institute of Nuclear Science and Technology, Islamabad, Pakistan.
Samina
S
Roohi
Department of Zoology, Government College Woman University, Faisalabad, Pakistan.
Saira
S
Hina
Isotope Production Division, Pakistan Institute of Nuclear Science and Technology, Islamabad, Pakistan.
Sajid
S
Mehmood
Pakistan Institute of Engineering and Applied Sciences, Islamabad, Pakistan.
Muhammad
M
Sohaib
Punjab Institute of Nuclear Medicine, Faisalabad, Pakistan.
Tania
T
Jabbar
D000818:Animals; D002851:Chromatography, High Pressure Liquid / Q000592:standards; D002855:Chromatography, Thin Layer / Q000592:standards; D004355:Drug Stability; D004586:Electrophoresis / Q000592:standards; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007553:Isotope Labeling; D007612:Kanamycin / Q000097:blood / Q000737:chemistry / Q000378:metabolism*; D008187:Lutetium / Q000737:chemistry; D008297:Male; D051379:Mice; D011786:Quality Control; D011817:Rabbits; D011868:Radioisotopes; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000097:blood / Q000737:chemistry / Q000378:metabolism* / Q000592:standards; D013696:Temperature; D014018:Tissue Distribution; D051598:Whole Body Imaging
D011868:Radioisotopes; D019275:Radiopharmaceuticals; D007612:Kanamycin; D008187:Lutetium
177Lu-kanamycin; HPLC; biodistribution; electrophoresis; quality control; radiolabeling; scintigraphy