OBJECTIVE To prepare osthole(OST)nanocrystallization and evaluate its characterization.METHODS OST-NSs were prepared by a media grinding method,and the average particle size and polydispersity index(PDI)were used as indicators to optimize the formulation and process parameters.The crystal morphology,crystal form,and interaction between OST-NCs and stabiliz-ers were characterized.Their surface wettability,equilibrium solubility,and in vitro dissolution in various media were investigated,and the f2 value was used to evaluate the similarity of the dissolution curves.RESULTS The formulation and process parameters for pre-paring OST-NCs were as follows:OST(3％):PVP-VA64,sodium deoxycholate 25∶5∶1,the volume ratio of grinding beads(0.4-0.6 mm)to OST suspension was 2∶1,and it was ground at 450 r·min-1 for 70 min,and 9％mannitol was used as a lyophilized protective agent to prepare OST-NCs.The stability of OST-NCs decreases with increasing temperature.After reconstitution,the particle size of OST-NCs was(354.2±9.857)nm,the PDI was(0.259±0.023),and the Zeta potential was(-22.2±0.896)mV.OST-NCs basically maintain the rod-shaped crystal structure.There is no interaction between OST and the stabilizer.The surface wetta-bility of OST-NCs is better than that of OST and its physical mixture.The equilibrium solubility of OST-NCs in pure water is 231％that of OST.Among the six dissolution media,the dissolution rate and cumulative dissolution of OST-NCs were significantly better than those of OST and its physical mixture.Additionally,the f2 values for the physical mixtures were greater than 50,whereas those for OST-NCs were less than 50,as compared with the dissolution curves of OST.CONCLUSION The results show that the reproducibility of OST-NCs is good during their preparation.The grinding temperature should be reduced,and the grinding time should be optimized.The dissolution behavior of OST-NCs is significantly different from that of OST.The reduction of particle size is the main reason for the improved water solubility of OST-NCs.These results suggest that the nanocrystallization strategy based on media grinding can effectively improve the water solubility and hydrophobicity of OST and has a good application prospect in the development of new OST drugs.
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