Background: Solubility properties of drugs intensify a crucial role during the formulation development process. Aqueous solubility is one of the most significant factors concerning drug bioavailability analysis. Cyclodextrins [CDs] are supportive, competent excipients, required an ever-rising way to disguise unwanted pharmaceutical characteristics, exclusively poor aqueous solubility. Main Text: CDs are actively useful in medicinal industries for copious purposes, including improving drug solubility, safety, physicochemical stability, and bioavailability. Different solubility enhancement methods can resolve several approaches to trouble insolubility. Conclusions: Among all, the reported one complexation technique has been incorporated as one of the imperative and the exigent concept, to enhance the solubility of poorly water-soluble drugs. The standard CDs and their explicit derivatives are quite essential in enabling pharmaceutical excipients, which improve the aqueous solubility of poorly soluble drugs, raise the permeability of drugs through the biological membranes, and advances the drug dissolution rate and bioavailability. This review discusses some of the findings and broad applications of CDs and their derivatives in various drug delivery areas. This review also addresses the aspects regarding the new CD-based therapeutics, possible future uses and issues, and regulatory perspective in the modern scenario.