Nanoparticles based drug delivery systems showing greater potential in various biomedical applications to deliver the drugs/bioactive molecules in controlled manner to the targeted site. Polycaprolactone, biodegradable polyester, owing its tailorable properties, various forms of polycaprolactone are used as drug carrier for a range of biomedical applications. Nanoprecipitation is a simple method to prepare the polycaprolactone nanoparticles to improve the bioavailability and therapeutic potential of various drugs/bioactive molecules. This short review focused on the preparation of polycaprolactone nanoparticles using nanoprecipitation method, nanoparticles-drug formulations and its use in various drug delivery applications.