Small interfering RNA (siRNA) is emerging as a class of therapeutic with extremely high potential, particularly in the field of oncology. Despite this growing interest, further understanding of how siRNA behaves in vivo is still required before significant uptake into clinical application. To this end, many molecular imaging modalities have been utilised to gain a better understanding of the biodistribution and pharmacokinetics of administered siRNA and delivery vehicles. This highlight aims to provide an overview of the current state of the field for preclinical imaging of siRNA delivery.