In recent years, poorly water-soluble drug candidates in the drug development pipeline have been a challenging issue for the pharmaceutical industry. Many delivery systems, such as nanocrystals, cocrystals, nanoparticles, and amorphous solid dispersions (ASDs) have been developed to overcome these problems. A large number of methods are utilized to realize the above delivery systems. Among all the preparation methods, the antisolvent coprecipitation method is a relatively simple, cost-effective method, offering many advantages over conventional methods. An overview of recent developments for each solubility enhancement approach using the antisolvent coprecipitation method is presented. This current review details a comprehensive overview of the antisolvent coprecipitation process and its properties, as well as the fundamentals for enhancing the solubility and bioavailability of poorly water-soluble drugs by nanotization, polymorph control with polymers and/or surfactants. Furthermore, this review also presents insights into the factors affecting the antisolvent coprecipitation process.