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。 OBJECTIVE: To study the in vitro release characteristics and irritation of encapsulated liposome-encapsulated liposomes in situ of sirolimus ocular. Methods: The release mechanism was studied by membraneless dissolution method, the release curve was fitted and analyzed. The Draize score combined with histological examination was used to evaluate the irritation to rat cornea. Results: There was a significant correlation between dissolution and in vitro release of the preparation. Slit lamp observation and histological examination showed no damage to the cornea. In vitro dissolution behavior and release behavior follow the zero-order kinetic equation, gel dissolution is to determine the main factor of drug release. Conclusion: The gel has good biosafety and deserves further study.