In vivo behaviors of meloxicam nanocrystals by intravenous administration are not significantly affected by stabilizers

Nanocrystals (NCs) are considered as an effective strategy for the formulation of intravenous injections for poorly water-soluble drugs, despite they are metastable dispersions. Typically, stabilizers are essential for the maintenance of physical stability, and they are important compositions for NCs. However, whether the stabilizers have impacts on the in vivo behaviors of NCs after intravenous injection are unknown. In this study, three meloxicam NCs (MLXNCs) were each formulated with a different steric stabilizer (PEG 400, lecithin and PVP-K17). The developed MLXNC PEG , MLXNC Lec and MLXNC PVP all had particle size of about 250 nm and shared the same crystal form. All three formulations had similar pharmacokinetic profiles and therapeutic efficacy, with no statistically significant differences. Overall results provided evidence that stabilizers have negligible effects on the in vivo behaviors of intravenous NCs and stress the importance of physical stability for formulation development.