Multidisciplinary research has been conducted on novel drug delivery technologies to maximize therapeutic advantages while curtailing undesirable reactions. Drugs under BCS Class II often have a low bioavailability because the dissolution phase limits the absorption efficiency. In this review, risperidone was used as a pharmacological model to examine the impact of solubility enhancement at the primary administration site for such pharmaceuticals. For tackling drug-related pertains like disease diagnostics, therapy, and prophylactic measures at the cellular or molecular levels, implementing nanocarriers in therapeutics has significant potential. The comprehensive pharmaceutical compositions of risperidone nano-microparticles that have been developed to alleviate psychosis are highlighted in the study, which also illustrates potential future developments in such domains.