| 引用本文: | 王雪莹,闫淑静,牛若惠,刘运霄,高晓黎.结合雌激素阴道用脂质体温敏凝胶的制备与性质考察[J].中国现代应用药学,2022,39(8):1059-1066. |
| WANG Xueying,YAN Shujing,NIU Ruohui,LIU Yunxiao,GAO Xiaoli.Preparation and Property Evaluation of Conjugated Estrogen Vaginal Liposome Thermosensitive Gel[J].Chin J Mod Appl Pharm(中国现代应用药学),2022,39(8):1059-1066. |
|
| 摘要: |
| 目的 制备结合雌激素阴道用脂质体温敏凝胶，考察其体外释放、流变学及阴道滞留等性质。方法 采用Box-Behnken响应面法优化脂质体处方；冷溶法制备结合雌激素脂质体温敏凝胶；用Franz扩散池考察体外释放性质；用流变仪进行剪切速率扫描、温度扫描、角频率扫描；用荧光成像法考察阴道滞留性。结果 以包封率为指标筛得结合雌激素脂质体最优处方：大豆磷脂与胆固醇用量分别为0.123 6 g与0.030 0 g(4.12∶1.00)，脂类与原料药用量分别为0.153 6 g与0.021 6 g(7.11∶1.00)，水化介质3.67 mL，包封率为(93.99±0.92)%；48 h累积释放率为(77.82±0.75)%；胶凝温度为(33.0±0.5)℃；胶凝后相变为半固体，流变学性质显著变化；IR820标记的脂质体温敏凝胶在昆明小鼠阴道内具有较高荧光强度且下降速率较慢。结论 结合雌激素脂质体温敏凝胶制备工艺可行，可在体温条件相变并延长在阴道的滞留时间。 |
| 关键词: 结合雌激素 脂质体 温敏凝胶 流变学 阴道滞留性 |
| DOI：10.13748/j.cnki.issn1007-7693.2022.08.009 |
| 分类号:R943 |
| 基金项目:新疆维吾尔自治区重点科技专项项目(2017A01002) |
|
| Preparation and Property Evaluation of Conjugated Estrogen Vaginal Liposome Thermosensitive Gel |
|
WANG Xueying1, YAN Shujing1, NIU Ruohui1, LIU Yunxiao1, GAO Xiaoli1,2
|
|
1.College of Pharmacy, Xinjiang Medical University, Urumuqi 830054, China;2.Xinjiang Key Laboratory of Active Components and Drug Release Technology for Natural Medicines, Urumuqi 830054, China
|
| Abstract: |
| OBJECTIVE To optimize conjugated estrogen liposome thermosensitive gel for vaginal drug delivery and evaluate its properties. METHODS Box-Behnken design and response surface methodology was used to optimize the formulation of liposome. The thermosensitive gel was prepared by cold solution method. Franz diffusion cell was employed for the in vitro release study. Shear rate scanning, temperature scanning and frequency scanning were performed by the rheometer. Vaginal retention was investigated by florescence imaging. RESULTS The optimal formulation contained 0.030 0 g cholesterol and 0.123 6 g lecithin(1.00:4.12), 0.021 6 g API and 0.153 6 g lipid(1.00:7.11), 3.67 mL PBS as hydrated medium. The entrapment efficiency was(93.99±0.92)% and the gelatination temperature was(33.0±0.5)℃. The in vitro accumulative release rates of liposome thermosensitive gel within 48 h was (77.82±0.75)%, the curve was well fitted with the Higuchi model. When the gelation temperature was reached, rheological properties changed significantly. IR820-labeled liposome thermosensitive gel showed high fluorescence intensity in vagina of KM mice and the intensity decreased slowly. CONCLUSION The formulation and preparation process of conjugated estrogen liposome thermosensitive gel are reasonable. It can transform into semisolid at gelation temperature and prolong retention in vagina. |
| Key words: conjugated estrogen liposome thermosensitive gel rheology vaginal retention |
