Different strategies are used to increase the bioavailability of pharmacoactive molecules because their low water solubility limits their pharmacological potential but the solubility parameter cannot be compromised. Low solubility pharmaceutically active molecules indicate a higher chance of drug development and innovation failure. One of the biggest challenges in the field of pharmaceutical formulations is improving the solubility and bioavailability of medications. The classification of biopharmaceutics states that drugs in classes II and IV (APIs) have poor solubility, lower bioavailability, and less dissolution. The complexation of active molecules, the use of cosolvents, crystal engineering techniques, drug nanocrystals, emulsion formation, micelles, microemulsions, nanomorph technology, particle size reduction technologies, pharmaceutical salts, prodrugs, the solid-state alternation technique, soft gel technology and solid dispersion methods are just a few of the technologies that are discussed in this article to improve the solubility of poorly water-soluble drugs. This review focuses on a number of other cutting-edge techniques for improving solubility and bioavailability, including drug conjugates, cyclodextrins, solid lipid nanoparticles, micronization, solid dispersions, nanosizing, and colloidal drug delivery systems. It does this by citing a number of pertinent research reports.