Most of the drugs administered through oral route have poor aqueous solubility and dissolution rate. Cyclodextrin and its derivates represent as pharmaceutical adjuvants to overcome this challenges and helps in development of stable formulation with enhanced bioavailability. Cyclodextrins are unique structure with versatile physicochemical properties which aids the pharmaceutical scientists to overcome drug delivery challenges for poorly aqueous soluble drugs. Cyclodextrin and its derivates are widely useful as solubilizers, assisting in preparation of various dosage forms such as liquid oral, solid, and parenteral preparations. Cyclodextrins interacts with appropriately sized guest molecules to form inclusion complex and enhance the aqueous solubility, physical chemical stability, and bioavailability of drugs. Through the various reported literatures, the review highlights the concept of cyclodextrin and its derivatives in enhancing solubility and bioavailability of poorly aqueous soluble drugs.