避蚊胺纳米硅缓释软膏的制备及驱蚊效果研究

Preparation and repellent effect of N, N-diethyl-m-toluamide loaded nanosilicon sustained release ointment

目的制备载避蚊胺的纳米介孔硅缓释软膏,考察其药剂学性质及驱蚊作用。方法纳米介孔硅材料吸附避蚊胺后液体石蜡包埋,制备成缓释软膏并研究其形态、稳定性及体外释放度。用改良Franz扩散池考察其经皮渗透行为。以驱蚊试验研究其缓释驱蚊作用。结果制备的载避蚊胺纳米硅缓释软膏呈乳白色半固体,避蚊胺载药量可达约25%,24 h体外累积释放低于60%,离体皮肤渗透显示药物主要滞留于皮肤表面,载避蚊胺纳米硅缓释软膏有效驱蚊时间超过12 h。结论纳米介孔硅可延缓避蚊胺的挥发,载避蚊胺纳米硅缓释软膏缓控释特性明显,驱蚊时间明显延长,并可能减少透皮吸收,提高用药安全性。

Objective To prepare N, N-diethyl-m-toluamide（DEET） loaded nano-silicon sustained release ointment, and determine its pharmaceutical properties and repellent effect. Methods Nano-silicon was embedded by liquid paraffin after adsorbing rich DEET, and was subsequently used in the preparation of DEET loaded nano-silicon sustained release ointment. The stability, morphology and in vitro release were examined. Percutaneous tests were done with improved Franz diffusion cells. Mosquito repellent test was used to study the effect of slow-release mosquito repellent. Results The characters of DEET sustained release ointment was milky white semisolid, with drug loading rate was about 25%. The in vitro cumulative release rate（24 h） of DEET was less than 60%. The in vitro skin penetration test showed that the main drug remained on the surface of the skin, and the effect of repellent last longer than 12 h. Conclusion DEET loaded nano-silicon sustained release ointment can delay the drug volatilization with sustained-release properties, enhance the mosquito repellent effect, reduce the transdermal absorption and improve the safety of DEET.