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目的考察雌二醇阴道用温敏性凝胶E2-VTG的体外释药特性及体内滞留性。方法采用冷法工艺制备E2-VTG。采用动态透析法和高效液相色谱-荧光法进行体外释放度研究。以新吲哚菁绿IR820为荧光标记物,ICR小鼠为受试动物,应用CRi Maestro小动物成像系统检测不同时间点温敏凝胶在受试小鼠阴道处的滞留情况。结果雌二醇温敏凝胶具有明显的缓释特征,24 h时药物累计释放率达到87%,释放模型拟合遵循Higuchi方程,推测雌二醇温敏凝胶主要通过扩散机制释药。NIR成像与荧光定量分析显示温敏凝胶在ICR小鼠阴道内滞留时间至少可达8 h。结论雌二醇温敏凝胶可延长药物在阴道内的滞留时间,延缓药物的释放。
Objective To investigate the in vitro release characteristics and in vivo retention of E2-VTG for estradiol vaginal gel. Methods E2-VTG was prepared by cold process. In vitro release studies were performed using dynamic dialysis and high performance liquid chromatography-fluorescence methods. The new indocyanine green IR820 was used as a fluorescent marker and ICR mice as test animals. The CRi Maestro small animal imaging system was used to detect the retention of temperature-sensitive gels in the vagina at different time points. Results The estradiol thermo-sensitive gel exhibited a sustained release profile. The cumulative release rate reached 87% at 24 h. The fit of the release model followed the Higuchi equation, suggesting that estradiol thermo-sensitive gel releases drug mainly through the diffusion mechanism. NIR imaging and fluorescence quantitative analysis showed that the thermo-sensitive gel retained vaginal in ICR mice for at least 8 h. Conclusion Estradiol thermo-sensitive gel can prolong the residence time of drug in vagina and delay the release of drug.