Preparation of nasal ethosome spray of geniposide and its nasal mucosa permeability in vitro / 中草药

ABSTRACT

Objective: To optimize the preparation technology of geniposide ethosome spray (GES) and to evaluate the regulation of its nasal mucosa permeability in vitro and nasal ciliotoxicity. Methods: Geniposide ethosomes were prepared by ethanol injection method. An central composite design-response surface method was used to optimize the related factors and technical parameters in the preparation of geniposide ethosomes with entrapment efficiency as evaluation index. Their physical properties were evaluated by the transmission electron microscope and photon correlation spectrometer. The isolated pig nasal mucosa was used to investigate the regulation of GES nasal mucosa permeability in vitro. The accumulated permeation amounts of geniposide aqueous solution, geniposide liposomes, and geniposide ethosomes were compared. In situ toad palate model was established to evaluate the effects of geniposide ethosomes on persistent vibration duration of toad palate cilia, so as to evaluate the cililary toxicity. Results: The average encapsulation percentage, particle size, drug loading, and Zeta potential of geniposide ethosomes were (65.80 ± 2.53)%, (173.40 ± 71.02) nm, (5.25 ± 0.15)%, and (-42.50 ± 8.27) mV, respectively. The accumulative permeation amount of geniposide ethosomes in 300 min was 23.39 μg/cm2, which was about 2.17 times of liposomes and 11.03 times of geniposide aqueous solution. Furthermore, the GES showed less mucociliary toxicity. Conclusion: The optimized formulation and preparation technology of geniposide ethosomes are rational. GES could significantly increase the mucosa permeability of geniposide and could be used for nasal administration.