眼用西罗莫司壳聚糖包覆脂质体-原位凝胶的体外释放特性与刺激性

目的:研究眼用西罗莫司壳聚糖包覆脂质体-原位凝胶的体外释药特性以及刺激性.方法:采用无膜溶出法研究其释放机制,对释放曲线进行拟合分析;Draize评分法结合组织学检查,评价其对大鼠角膜的刺激性.结果:该制剂的溶蚀度与体外释放度有明显相关性,裂隙灯观察和组织学检查对角膜均无损伤.体外的溶蚀行为与释放行为遵循零级动力学方程,凝胶溶蚀是决定药物释放的主要因素.结论:该凝胶具有良好的生物安全性,值得进一步研究.

In Vitro Release and Irritation of Ocular Sirolimus Chitosan-coated Liposomal In-situ Gels

Objective:To study the in vitro release and irritation of ocular sirolimus chitosan-coated liposomal in-situ gels.Method: The non-membrane model was applied to observe the drug release and gel erosion,and the release data were analyzed with fitted equations. Ocular irritation test was carried out based on the Draize method and histological examination.Result:A significant correlation was shown between the gel erosion and the drug release of ocular sirolimus chitosan-coated liposomal in-situ gels.Both slit lamp observation and histological examination showed no damage to the cornea.In vitro dissolution and release behavior were fitted the zeroorder kinetics equation,and the gel erosion was the major influencing factor in the drug release.Conclusion:The gels show promising biocompatibility and safety,which are valuable to be studied further.