Abstract Around forty percent of new chemical entities (NCEs) are reported to be poorly soluble in water. This translates to poor bioavailability and, thereby, limits the development of these molecules as drug candidates. It is suggested that nanoformulations of poorly-water soluble NCEs/Drugs are viable routes to increase the bioavailability of these molecules. The role of particle size in molecular dissolution is discussed. Different nanostructures that can incorporate poorly-water soluble NCEs/Drugs and which have been previously reported in the literature such as nanoemulsions, nanosuspensions and nanoscale NCE/Drug-Polymer composites are presented. Methods for the preparation of these nanostructures are discussed. Characterization techniques such as Powder X-Ray Diffraction (PXRD), Dynamic Light Scattering (DLS), Zeta Potential Measurement, Scanning Electron Microscopy (SEM), Transmission Electron Microscopy (TEM), Atomic Force Microscopy (AFM) and Differential Scanning Calorimetry (DSC) are discussed. Finally, an example of an NCE-Polymer Nanocomposite is presented.