本文選題：黃藤素　切入點：柔性納米脂質體　出處：《中國藥學雜志》2015年24期

【摘要】：目的制備黃藤素柔性納米脂質體(PFNL),并考察其藥劑學性質與體外透黏膜給藥的行為特點,為進一步應用奠定基礎。方法以薄膜分散法制備黃藤素柔性納米脂質體,采用魚精蛋白凝聚與高效液相色譜儀測定包封率,考察卵磷脂、膽固醇與丙二醇對脂質體包封率的影響;用透射電鏡(TEM)、光子相關光譜儀(PCS)與激光共聚焦顯微鏡(CLSM)評價脂質體的粒徑和結構;通過測定脂質體透過微孔濾膜的相對速率評價其變形性;用恒溫電導率法測定脂質體的凝聚速度常數(shù)(K)以評價其物理穩(wěn)定性。采用水平雙室擴散池考察黃藤素柔性納米脂質體通過豬陰道黏膜的給藥行為,并考察其對大鼠陰道組織中細胞因子SLPI、LF和SP-D表達的影響,與黃藤素普通脂質體(PCL)及其溶液劑(PL)進行對比。結果卵磷脂、膽固醇和丙二醇的質量分數(shù)分別為3%、0.02%、20%時,制備的黃藤素柔性納米脂質體對黃藤素的包封率為(78±2.13)%;黃藤素柔性納米脂質體為圓形或橢圓形的多層狀囊泡結構,粒徑為(185±19)nm,Zeta電位為(-53±2.27)m V,變形性為(79±5.75)%;黃藤素柔性納米脂質體K值始終低于黃藤素的普通脂質體的K值。6.0 h時,黃藤素柔性納米脂質體的藥物累積透過量分別為黃藤素的普通脂質體和其溶液劑的1.53與2.86倍,且藥物在陰道組織中的滯留量也高于黃藤素的普通脂質體和其溶液劑;黃藤素柔性納米脂質體不影響大鼠陰道組織中SLPI、LF和SP-D表達,組織切片未顯示異常。結論黃藤素柔性納米脂質體對黃藤素的包封率高、穩(wěn)定性好,能夠促進藥物通過陰道黏膜并在黏膜組織中形成藥物儲庫,對陰道安全無刺激,因此,可作為黃藤素陰道給藥的一種新型給藥載體。
[Abstract]:Objective to prepare Fibrauretinum flexible nano liposomes (PFNL), and investigate their pharmaceutical properties and in vitro transmucosal drug behavior characteristics, which lays a foundation for the further application of Fibrauretin. Preparation of flexible nano liposomes by thin film dispersion method, condensation and high performance liquid chromatography for determination of entrapment efficiency, effects of lecithin by protamine. Cholesterol and propylene glycol on liposomes; by transmission electron microscopy (TEM), photon correlation spectroscopy (PCS) and laser scanning confocal microscope (CLSM) evaluation of liposome size and structure; through the determination of liposome through the evaluation of the relative rate of membrane deformation; Determination of coagulation rate constants of liposomes with constant conductivity method (K) to evaluate the physical stability. The influences of Fibrauretin flexible nano liposomes by porcine vaginal mucosa drug delivery behavior by dual chamber diffusion cells, and examine the rat vaginal tissue 涓粏鑳?yōu)鍥犲瓙SLPI,LF鍜孲P-D琛ㄨ揪鐨勫獎鍝，

本文編號：1706040