One of the most common routes for drug administration is the oral route. It has many advantages like patient compliance, non-invasiveness and drug administration convenience. Oral administration accounts for over 60% of all established small-molecule medication products on the market. Oral drug absorption may be governed by many factors such as mucosal permeability, drug solubility and stability in the gastrointestinal tract. The trials to overcome these factors depend on understanding the biochemical, physicochemical, biological and metabolic barriers which affect the overall bioavailability of a drug. Enhancement of oral drug absorption can be achieved by many drug delivery systems and pharmaceutical technologies such as lipid-based carriers, micelles, nanocarriers, salt formation, solid dispersion, and complexation techniques using cyclodextrins. The strategies to improve the oral drug delivery will be discussed in details especially cyclodextrin complexation which is considered one of the most common strategies having great role in enhancing the oral drug delivery.