黄藤素柔性纳米脂质体的制备及体外透黏膜给药研究

发布时间：2018-04-03 16:43

  本文选题：黄藤素　切入点：柔性纳米脂质体　出处：《中国药学杂志》2015年24期

【摘要】：目的制备黄藤素柔性纳米脂质体(PFNL),并考察其药剂学性质与体外透黏膜给药的行为特点,为进一步应用奠定基础。方法以薄膜分散法制备黄藤素柔性纳米脂质体,采用鱼精蛋白凝聚与高效液相色谱仪测定包封率,考察卵磷脂、胆固醇与丙二醇对脂质体包封率的影响;用透射电镜(TEM)、光子相关光谱仪(PCS)与激光共聚焦显微镜(CLSM)评价脂质体的粒径和结构;通过测定脂质体透过微孔滤膜的相对速率评价其变形性;用恒温电导率法测定脂质体的凝聚速度常数(K)以评价其物理稳定性。采用水平双室扩散池考察黄藤素柔性纳米脂质体通过猪阴道黏膜的给药行为,并考察其对大鼠阴道组织中细胞因子SLPI、LF和SP-D表达的影响,与黄藤素普通脂质体(PCL)及其溶液剂(PL)进行对比。结果卵磷脂、胆固醇和丙二醇的质量分数分别为3%、0.02%、20%时,制备的黄藤素柔性纳米脂质体对黄藤素的包封率为(78±2.13)%;黄藤素柔性纳米脂质体为圆形或椭圆形的多层状囊泡结构,粒径为(185±19)nm,Zeta电位为(-53±2.27)m V,变形性为(79±5.75)%;黄藤素柔性纳米脂质体K值始终低于黄藤素的普通脂质体的K值。6.0 h时,黄藤素柔性纳米脂质体的药物累积透过量分别为黄藤素的普通脂质体和其溶液剂的1.53与2.86倍,且药物在阴道组织中的滞留量也高于黄藤素的普通脂质体和其溶液剂;黄藤素柔性纳米脂质体不影响大鼠阴道组织中SLPI、LF和SP-D表达,组织切片未显示异常。结论黄藤素柔性纳米脂质体对黄藤素的包封率高、稳定性好,能够促进药物通过阴道黏膜并在黏膜组织中形成药物储库,对阴道安全无刺激,因此,可作为黄藤素阴道给药的一种新型给药载体。
[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�缁嗚優鍥犲瓙SLPI,LF鍜孲P-D琛ㄨ揪鐨勫奖鍝，

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