An in situ gel system for nasal delivery of menthol: preparation and safety evaluation
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摘要: 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。Abstract: Objective To prepare an in situ gel system for nasal delivery of menthol and to evaluate the safety of this formulation. Methods Menthol in situ gel was prepared with deacetylatedgellan gum. The nasal mucocilia toxicities of this formulation was evaluated using in situ 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 rabbits. Skin allergic reaction was not found in guinea pigs. Conclusion The preparation of menthol in situ nasal gel with low ciliary toxicity was easily achieved. This gel has good physiological flexibility.The further investigation was warranted for this formulation as an intranasal drug delivery system.
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Key words:
- in situ gel /
- menthol /
- nasal drug delivery /
- deacetylatedgellan gum /
- safety
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[1] Takano K, Kojima T, Keira T, et al. A novel drug delivery system for the human nasal epithelium[J]. Adv Otorhinolaryngol, 2016,77:67-74. [2] Gu F, Ma W, Meng G, et al. Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone[J]. Acta Pharm, 2016,66(4):555-562. [3] Karavasili C, Fatouros D G. Smart materials: in situ gel-forming systems for nasal delivery[J]. Drug Discov Today, 2016,21(1):157-166 [4] 张 奕, 蒋新国. 鼻腔给药系统的鼻黏膜毒性及解决途径[J]. 中国医药工业杂志, 2001,32(7):323-327. [5] Xu X, Shen Y, Wang W, et al. Preparation and in vitro characterization of thermosensitive and mucoadhesive hydrogels for nasal delivery of phenylephrine hydrochloride[J]. Eur J Pharm Biopharm, 2014,88(3):998-1004. [6] 李彦林, 周云丰, 李 琳, 等. 平痤洗剂皮肤刺激和过敏性实验研究[J]. 中国中医药信息杂志, 2016,23(2):56-58. [7] 李 杰, 欧余航, 陈 强. 复方九节茶乳膏的抗炎镇痛及皮肤安全性的初步研究[J]. 西北药学杂志, 2016,(1):64-67. [8] Li X, Du L, Chen X, et al. Nasal delivery of analgesic ketorolac tromethamine thermo-and ion-sensitive in situ hydrogels[J]. Int J Pharm, 2015,489(1-2):252-260. [9] Osmalek T, Froelich A, Tasarek S,et al. Application of gellan gum in pharmacy and medicine[J]. Int J Pharm, 2014,466(1-2):328-340. -
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