The field of siRNA delivery has expanded rapidly over recent years, positioning siRNA as a powerful gene therapy tool for treating diverse diseases. Among the primary delivery approaches, siRNA bioconjugation stands out for its ability to enhance the pharmacological attributes of siRNA, while reducing stability-related toxicity and variability. This chapter presents an overview of the latest advancements in siRNA bioconjugation. It covers a range of conjugation approaches including those involving antibodies, peptides, aptamers, small molecules, lipidoids, cell-penetrating peptides, polymers, and nanoparticles. These bioconjugates, whether used independently or in combination with other compounds, have been shown to notably improve pharmacokinetics, extend biological half-life, and amplify targeting capabilities, all while ensuring effective gene silencing. These enhancements contribute to better therapeutic outcomes and reduce side effects. This chapter also highlights the critical role of conjugation techniques in maintaining the integrity, stability, and controlled release of siRNA bioconjugates and discusses the challenges associated with these methods.