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异硫氰酸荧光素(FITC)标记的模型化合物通过颊黏膜上皮的扩散速率和转运途径

Diffusion rates and transport pathways of fluorescein isothiocyanate (FITC)-labeled model compounds through buccal epithelium.

作者信息

Hoogstraate A J, Cullander C, Nagelkerke J F, Senel S, Verhoef J C, Junginger H E, Boddé H E

机构信息

Leiden/Amsterdam Center for Drug Research, Leiden University, The Netherlands.

出版信息

Pharm Res. 1994 Jan;11(1):83-9. doi: 10.1023/a:1018949828548.

Abstract

The aim of this study was to characterize transport of FITC-labeled dextrans of different molecular weights as model compounds for peptides and proteins through buccal mucosa. The penetration of these dextrans through porcine buccal mucosa (a nonkeratinized epithelium, comparable to human buccal mucosa) was investigated by measuring transbuccal fluxes and by analyzing the distribution of the fluorescent probe in the epithelium, using confocal laser scanning microscopy for visualizing permeation pathways. The results revealed that passage of porcine buccal epithelium by hydrophilic compounds such as the FITC-dextrans is restricted to permeants with a molecular weight lower than 20 kDa. The permeabilities of buccal mucosa for the 4- and 10-kDa FITC-dextran (of the order of 10(-8) cm/sec) were not significantly different from each other or from the much smaller compound FITC. The confocal images of the distribution pattern of FITC-dextrans showed that the paracellular route is the major pathway through buccal epithelium.

摘要

本研究的目的是将不同分子量的异硫氰酸荧光素(FITC)标记葡聚糖作为肽和蛋白质的模型化合物,表征其通过颊黏膜的转运情况。通过测量经颊通量,并使用共聚焦激光扫描显微镜观察渗透途径,分析荧光探针在上皮中的分布,研究了这些葡聚糖在猪颊黏膜(一种与人类颊黏膜类似的非角化上皮)中的渗透情况。结果显示,亲水性化合物如FITC标记葡聚糖通过猪颊上皮的过程仅限于分子量低于20 kDa的渗透物。颊黏膜对4 kDa和10 kDa FITC标记葡聚糖的渗透率(约为10^(-8) cm/秒)彼此之间以及与小得多的化合物FITC相比均无显著差异。FITC标记葡聚糖分布模式的共聚焦图像表明,细胞旁途径是通过颊上皮的主要途径。

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