In the realm of pharmaceutical advancement, the transformative prowess of nanotechnology shines through its precision-targeted drug delivery and amplified therapeutic effects. This paper ventures into the realm of radiolabeling techniques for unraveling the intricate choreography of drug kinetics within the bloodstream which encompass the delicate stages of absorption, distribution, metabolism, and excretion. Through the magical lens of the radiolabel, a real-time spectacle unfolds, providing invaluable insights into the safety and efficacy of nanomedicine interventions. Amid the labyrinthine complexities of drug-organism interactions and the lack of universal protocols for nanomedicine preparation, radiolabeling technology has emerged as a guiding constellation. The paper systematically assesses the methods commonly employed for pharmacokinetic studies, delves into the manifold advantages and techniques of radiolabel methods within the nanomedicine landscape, closely examines their application across a spectrum of pharmacokinetic studies and thoughtfully addresses the challenges they may pose. Embark on this illuminating odyssey—a journey that peers into the microcosm of nanomedicine, deciphering its dynamic interplay within the bloodstream through the luminary insights of radiolabeled tracing techniques.