Formulation and Evaluation of Aprepitant Nanosuspension by Nano Precipitation Techniques

Objective: The majority of new chemical substances generated by the drug development process are poorly water-soluble or lipophilic. Formulation of a poorly water-soluble substance is a difficult task for the pharmaceutical industry. It is widely acknowledged that using nanosuspension in drug administration enhances the drug’s solubility, dissolution, and ultimately bioavailability. This study aimed to examine the particle sizes of nanosuspensions made by nanoprecipitation techniques and improve their effectiveness. Methods: Aprepitant’s nanosuspension has been produced by nanoprecipitation techniques. The particle size, polydispersity index, along zeta potential of the produced nanosuspensions were measured. The optimized nanosuspension has been investigated further for solubility, dissolution, surface morphology, FT-IR, DSC as well as stability studies. Results: The combination of tween 80 and poloxamer 188 as stabilizer resulted in the preparation of an optimized nanosuspension (F9) with a particle size of 738 nm, polydispersity index 0.236, zeta potential -15.1 mV and an improved solubility and dissolution profile compared to pure drugs. Positive performance improvement was observed in the solubility and dissolution studies. The crystallinity changed upon nanosizing, as demonstrated by the SEM, FT-IR and DSC analysis. Conclusion: The nanoprecipitation method was effective in producing a stable Aprepitant nanosuspension with improved solubility and dissolution rate.