Effect of bile salts on nasal permeability in vitro.
Effect of bile salts on nasal permeability in vitro.
复制标题
胆汁盐对体外鼻通透性的影响。
DOI：
10.1002/jps.2600761206
复制
发表时间：
1987
影响因子：
3.8
通讯作者：
Jackson,RT
中科院分区：
文献类型：
--
作者：
Hersey,SJ;Jackson,RT
将从狗或兔切除的鼻粘膜作为平板固定在体外室中。通过测量放射性标记的示踪化合物、水、蔗糖、聚乙二醇和八肽胆囊收缩素的单向通量来评估渗透性。根据通量计算的渗透系数表明，鼻粘膜对水溶性化合物具有中度渗透性，并与回肠或胆囊进行比较。在粘膜浴溶液中加入0.5%脱氧胆酸钠可使蔗糖或八肽胆囊收缩素的渗透性迅速增加4 - 5倍。渗透性的增加是双向的，不会被冲洗逆转，并伴有表面上皮层广泛损失的组织学证据。这些结果表明，胆汁盐通过去除上皮细胞而增强鼻渗透性，上皮细胞构成主要的渗透性屏障，而不是引起粘膜细胞的化学修饰。这反对使用胆汁盐来增强患者的鼻腔药物吸收。
Nasal mucosa excised from dogs or rabbits was mounted as a flat sheet in an in vitro chamber. The permeability was assessed by measuring the unidirectional flux of the radiolabeled tracer compounds, water, sucrose, polyethylene glycol, and cholecystokinin octapeptide. The permeability coefficients calculated from the fluxes indicate that the nasal mucosa is moderately permeable to water‐soluble compounds and compares with ileum or gallbladder. The addition of 0.5% sodium deoxycholate to the mucosal bathing solution caused a rapid, four‐ to fivefold increase in permeability to sucrose or cholecystokinin octapeptide. The increase in permeability was bidirectional, was not reversed by washing, and was accompanied by histological evidence of extensive loss of the surface epithelial layer. These results indicate that bile salts enhance nasal permeability by removing the epithelial cells, which constitute a major permeability barrier, rather than causing a chemical modification of the mucosal cells. This argues against the use of bile salts to enhance nasal drug absorption in patients.