In vitro evaluation of diosgenin nanosuspensions with different particle sizes / 中草药

ABSTRACT

Objective To investigate the effect of particle size on the physicochemical properties, aqueous solubility and physical stability of diosgenin nanosuspensions (DSG-NS). Methods DSG-NS with different particle sizes were prepared using the milling bead with the diameter of 0.5 (DSG-NS0.5) and 1.0 mm (DSG-NS1.0) by media milling method using the combination of Pluronic F127 and sodium dodecyl sulfate as stabilizer, respectively. The DSG-NS were solidified by freeze drying method. The physicochemical properties of DSG-NS were characterized in term of particle distribution, scanning electron microscope, X-Ray diffraction and Fourier transform infrared spectroscopy. The aqueous solubility of DSG-NS with two particle size was compared by equilibrium solubility and dissolution rate. Results The particle sizes of the DSG-NS1.0 and DSG-NS0.5 prepared in this paper were (762.5 ± 18.4) and (342.8 ± 7.3) nm with the polydisperson index (PDI) of 0.435 ± 0.087 and 0.170 ± 0.018, respectively. The re-dispersed freeze drying products had particle sizes of (919.0 ± 27.2) and (458.0 ± 10.3) nm with the polydisperson index of 0.521 ± 0.094 and 0.298 ± 0.021, respectively. Both DSG-NS1.0 and DSG-NS0.5 had an irregular rod-shape or flake without any aggregates. The DSG retained its original crystalline state during the manufacturing process of DSG-NS1.0 and DSG-NS0.5. The solubilities of freeze drying DSG-NS1.0 and DSG-NS0.5 were (5.094 ± 2.083) and (26.121 ± 10.286) μg/mL. The accumulated dissolution rate of freeze drying DSG-NS1.0 and DSG-NS0.5 was 36.1% and 64.9% in 60 min, respectively. The particle size presented significant increase in 10 d for the DSG-NS1.0, whereas it had no change in 30 d for DSG-NS0.5. However, the particle size and distribution of the freeze drying DSG-NS1.0 and DSG-NS0.5 were stable during the storage of 3 month. Conclusion The reduction of particle size had no effect on the changing of morphology and original crystalline state and contributed to the improvement of solubility, dissolution rate and physical stability of DSG-NS.