THE EFFECTS OF PERMEATION ENHANCERS ON THE SURFACE-MORPHOLOGY OF THE RAT NASAL-MUCOSA - A SCANNING ELECTRON-MICROSCOPY STUDY

被引:72
作者
ENNIS, RD [1 ]
BORDEN, L [1 ]
LEE, WA [1 ]
机构
[1] CALIF BIOTECHNOL INC,DEPT DRUG DELIVERY,2450 BAYSHORE PKWY,MT VIEW,CA 94043
关键词
bile salt; fusidic acid; morphology; nasal delivery; nasal mucosa; permeation enhancer; scanning electron microscopy; surfactant; toxicity;
D O I
10.1023/A:1015856430657
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A rat model has been developed to compare relative morphological changes in the nasal mucosa after exposure to potential membrane permeation enhancers. Scanning electron microscopy was used to characterize gross structural and specific cellular changes following exposure. Micrographs of the rat nasal mucosa were scored in four categories: (1) mucosal surface integrity, (2) ciliary morphology, (3) mucus/extracellular debris, and (4) presence of red blood cells. The order of increasing morphological damage resulting from a 5-min exposure to each surfactant was 0.5% Solulan C-24 ≈ 0.5% Solulan C-24/0.5% sodium tauro-24,25-dihydrofusidate (STDHF) < 0.5% STDHF < 1.0% STDHF ≪ 1.0% Laureth-9 < 1.0% sodium taurodeoxycholate ≈1.0% sodium deoxycholate. The changes observed in the mucosal morphology after exposure to the various surfactants are in general agreement with data in the literature. This model is able to compare rapidly the relative morphological effects on the mucosal membrane of different nasal formulations. © 1990, Plenum Publishing Corporation. All rights reserved.
引用
收藏
页码:468 / 475
页数:8
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