Synthesis and in vitro evaluation of 99mTc radiolabeled lapatinib (LPT) and its PLGA formulation

• Published in: Journal of radioanalytical and nuclear chemistry Vol. 333; no. 2; pp. 665 - 672
• Main Authors: Gokulu, Sevki Goksun, Karatay, Kadriye Busra, Bilgi, Ahmet, Kayas, Cansu, Yildirim, Nuri, Kilcar, Ayfer Yurt, Muftuler, Fazilet Zumrut Biber, Terek, Mustafa Cosan, Akman, Levent
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.02.2024; Springer Nature B.V
• Subjects: Chemistry; Chemistry and Materials Science; Diagnostic Radiology; Glycolic acid; Hadrons; Heavy Ions; Inorganic Chemistry; Kinases; Nuclear Chemistry; Nuclear Physics; Physical Chemistry; Radioactive tracers; Radiochemistry; Technetium; Technetium isotopes; Tyrosine; Technetium-99 m; Cervix adenocarcinoma (HeLa); Lapatinib (LPT); Poly(lactic-co-glycolic acid) (PLGA); Human ovarian (MDAH-2774); Tc; Human breast adenocarcinoma (MDA-MB-231)
• ISSN: 0236-5731; 1588-2780
• DOI: 10.1007/s10967-023-09292-7

Lapatinib-(LPT) is a dual tyrosine kinase inhibitor that has important effects on the targeted therapy of various tumours. The current study is aimed to use a novel tracer strategy including Technetium-99 m-( 99m Tc) radiolabeled LPT and its poly(lactic-co-glycolic acid)-(PLGA) encapsulated formulation-(LPT-PLGA). In vitro bioaffinity of the [ 99m Tc]Tc-LPT and [ 99m Tc]Tc-LPT-PLGA was evaluated by using cell culture methods on human breast adenocarcinoma (MDA-MB-231), cervix adenocarcinoma and human ovarian (MDAH-2774) cancer cell lines. Radiochemical yield were over 95% and both compounds were examined high incorporation values on HeLa and MDAH cell lines. Current results may contribute to develope as the encapculated agents including radiotracer.