Cyclodextrins (CDs) have garnered significant attention in various scientific and industrial fields due to their unique ability to form inclusion complexes with a wide range of guest molecules. This review comprehensively explores the latest advancements in cyclodextrin chemistry, focusing on the synthesis and characterization of cyclodextrin derivatives and their inclusion complexes. This review examines the biological activities of cyclodextrins, highlighting their pharmacological properties and pharmacokinetics, and discussing their promising applications in drug delivery systems. Furthermore, the industrial utilization of cyclodextrins, including their role in nanomaterials and nanostructured coatings, as well as their potential in environmental remediation, are explored. The present research also addresses the critical aspect of toxicity, particularly concerning cyclodextrin inclusion complexes, providing an overview of the current understanding and safety considerations. Through a multidisciplinary approach, the aim is to present a complete view of cyclodextrins, underscoring their versatility and impact across various domains.