薄荷脑鼻腔原位凝胶剂的制备及安全性研究

An in situgel system for nasal delivery of menthol:preparation and safety evaluation

目的制备薄荷脑鼻用原位凝胶剂,并对其进行安全性考察。方法采用去乙酰结冷胶为材料制备离子敏感性原位凝胶。考察鼻腔原位凝胶对蟾蜍鼻黏膜纤毛的毒性及大鼠鼻黏膜的影响;并进行家兔皮肤刺激实验和豚鼠皮肤过敏实验,观察皮肤反应并评分。结果薄荷脑鼻用原位凝胶剂对蟾蜍鼻黏膜纤毛无显著毒性,对大鼠鼻黏膜形态及细胞分化无显著影响;对家兔完整皮肤无刺激作用,豚鼠皮肤无过敏反应。结论薄荷脑鼻用原位凝胶剂具有制备工艺简便、纤毛毒性低、生理相容性好的优点,开发为经鼻给药系统可行性良好。

Objective To prepare an insitu gel system for nasal delivery of menthol and to evaluate the safety of this for - mulation . Methods Menthol in situ gel was prepared with deacetylatedgellan gum . The nasal mucocilia toxicities of this for - mulation was evaluated using insitu toad palate model .Guinea pig skin sensitization test and the rabbit skin irritation test were conducted . Skin allergy and irritation reaction were monitored and scored . Results No significant effect on nasal mucosa ciliary movement and the morphology of rat nasal mucosa were observed .The formulation did not induce any dermal irritation in rab - bits . Skin allergic reaction was not found in guinea pigs .Conclusion The preparation of menthol insitu nasal gel with low cili-ary toxicity was easily achieved . This gel has good physiological flexibility .The further investigation was warranted for this for - mulation as an intranasal drug delivery system .