The majority of the pharmaceutically active chemical moieties represent a challenge in their formulation. Most of these drugs have intricate bioavailability issues either related to their low solubility or permeability. Many problems may arise during formulations such as pH dependent ionization, poor drug solubility, limited absorption, unpredicted bioavailability, degradation, metabolism, and cellular efflux. Poor aqueous solubility is a determinate criterion, during formulation and Biopharmaceutical Classification System (BCS) categorization. Among the most important approaches to enhance solubility, the Lipid-Based Drug Delivery Systems (LBDDS). The strategies involving lipid incorporation was a revolutionary step and included: vesicular systems, lipid particulate systems and emulsions.