Bioactive glass (BG) being bioactive, biocompatible, and osteoconductive has been explored as an oral drug carrier. Herein, after bio‐inspired synthesis, radiolabeling of BG is carried out with Technetium (99mTc) to study its biodistribution and analyze its physico‐chemical characteristics. The particles formed were found to be bioactive due to the formation of hydroxyapatite. An in‐vitro cell proliferation assay confirmed the cytocompatibility of BG against Caco‐2 and U2OS cell lines. The cellular uptake studies of BG for caco‐2 cell lines confirms intracellular nanoparticle transport making it suitable oral drug carrier. The radiolabeling efficiency was monitored in‐vitro at different pH levels of gastrointestinal tract (GI) at different time intervals and the efficacy of radiolabeled BG was found to be substantial. Finally, they were orally ingested in a rat model to investigate its biological diffusion. As depicted by SPECT images (Single photon emission computerized tomography), radiolabeled BG were found to be confined in the intestinal (abdomen) region. The goal of this study is to highlight the application of BG as oral drug carrier for the sustained targeted drug delivery to minimize the drug dosage with the least possible side effects.