Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system and is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response. Poorly water-soluble drugs after oral administration often require high doses in order to reach therapeutic plasma concentrations. The bioavailability of an orally administered drug depends on its solubility in aqueous media over different pH ranges. The insufficient dissolution rate of the drug is the limiting factor in the oral bioavailability of poorly water soluble compounds. Various techniques are used for the improvement of the aqueous solubility, dissolution rate, and bioavailability of poorly water soluble drugs include micronization, chemical modification, pH adjustment, solid dispersion, complexation, co-solvency, micellar solubilization, hydrotropy etc. The purpose of this review article is to describe the techniques of solubilization for the attainment of effective absorption with improved bioavailability.