Quantum dots (QDs), also known as quantum nanodots or colloidal nanocrystals, possess unique visual and electrical properties that have enabled various applications in biomedicine, particularly in drug delivery. Quantum dots offer significant advantages, such as a high surface area for drug attachment, the ability to modify solubility and drug release patterns, and the potential for targeted delivery. This review covers various aspects of QD research, including their synthesis, properties, and the challenges associated with their use. Key challenges include concerns about QD toxicity, stability, and environmental impact. Additionally, the article discusses using quantum dot-Förster resonance energy transfer (QD-FRET) to study in vivo drug release kinetics. This capability is essential for evaluating the performance of QDs as drug carriers and understanding their interactions within biological systems. In summary, while QDs present promising opportunities for advancing drug delivery mechanisms, ongoing research is necessary to mitigate toxicity concerns and enhance their biocompatibility, paving the way for their clinical application in targeted therapies.