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-(99mTc) radiolabeled LPT and its poly(lactic-co-glycolic acid)-(PLGA) encapsulated formulation-(LPT-PLGA). In vitro bioaffinity of the [99mTc]Tc-LPT and [99mTc]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.