Résumé
OBJECTIVE： To prepare the Peppermint oil moisturizing microemulsion for nasal mucosa and survey its mucosal adhesion and cilia toxicity. METHODS： The polyoxyethylene hydrogenated castor oil was used as emulsifier to prepare the Peppermint oil moisturizing microemulsion for nasal mucosa， and the preparation technology was optimized on the basis of comprehensive score by orthogonal design. The microemulsion was characterized and the menthol content was determined by GC. The mucosal adhesion was evaluated by measuring the transport rate by cilia in vivo， and the cilia toxicity of microemulsion was evaluated by measuring the sustained movement time of cilia in vitro. RESULTS： The optimal preparation technology of self-made microemulsion was to firstly disperse the peppermint oil and the emulsifier， then add anhydrous ethanol， edible glycerin and distilled water， and stir at 1 200 r/min for 2 h. The average contents of menthol in the three batches of the microemulsion were 2.682， 2.507 and 2.496 mg/mL （RSD＝2.89％，n＝3）， respectively. The cilia transport rates in vivo were （0.65±0.01）， （0.78±0.03）and （0.92±0.04） cm/min in high-dose， medium-dose， and low-dose groups of self-made microemulsion （2.561， 0.256， 0.128 mg/mL of menthol） respectively， which were significantly lower than normal saline group and compound menthol nasal droups （P＜0.05）. The cilia movement time in vitro were（206.7±4.9）， （226.0±13.5）， （269.3±12.9）min， which were significantly longer than sodium deoxycholate group （P＜0.05）. CONCLUSIONS： The preparation technology of self-made microemulsion is easy-to-handle and controllable in quality. The prepared microemulsion shows good mucosal adhesion without cilia toxicity．
Résumé
Objective:To evaluate the nasal safety of gastrodin nasal temperature-sensitive in situ gel through the studies on cilia toxicity in toads and mucosal irritation in rats. Methods:The toads were randomly divided into four groups, saline group, gastrodin in situ gel group, blank gel matrix group and sodium deoxycholate group, and the cilia toxicity was observed in vivo by a toad palate meth-od. The rats were randomly divided into three groups, saline group, gastrodin in situ gel group and blank gel matrix group, and the mucosal irritation was studied in rats through the observation of nasal mucosal pathological changes and behavioral indices. Results:Compared with the saline group, gastrodin in situ and blank gel matrix showed no notable effect on the cilia movement function in toads, and the effect on cilia movement of sodium deoxycholate showed statistically significant difference when compared with that of sa-line, gastrodin in situ gel and blank gel matrix (P0. 05), and after the 2-day withdrawal, that in the gastrodin in situ gel group and blank gel matrix group decreased significantly when compared with that at the last administration (P0. 05). The number of inflammatory cells in the nasal mucosa in the gastrodin in situ gel group and blank gel matrix group increased complicated with congestion and cilia falling off, and after the with-drawal, the mucosal morphology in the three groups showed no significant difference. Conclusion:The local application of gastrodin in situ gel has high security, which is valuable to be studied further.