Evaluation of mucosal damage of surfactants in rat jejunum and colon

A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P‐glycoprotein activity in vitro

“…25,26 However, several serious anaphylactic reactions have been observed in humans and animals following parenteral and, more rarely, oral administration of formulations containing polyoxyethylene castor oil derivatives such as Cremophor EL. 26 Although studies have been performed to assess the effects of these excipients on gross morphological changes and on animal toxicity, [24][25][26][27][28][29] little research has investigated the possible effects of these excipients in vitro until recently. [15][16][17][30][31][32] Previous studies in our laboratory 16,17 have shown that Cremophor EL and Tween 80 do not disrupt the passive diffusion of solutes across the paracellular or transcellular pathway of Caco-2 cell monolayers at concentrations < 10% and 1% (w/v), respectively.…”

Improvement of Intestinal Absorption of Macromolecules by Nitric Oxide Donor

“…However, in most cases, the enhancement of drug absorption was accompanied by mucosal injury due to the enhancer. 8,[22][23][24] Local toxicities of absorption enhancers have been assessed by various methods, including hemolysis, 25 protein elution, 4,16 phospholipid elution, 4,16 LDH elution, 26,27 and morphological observation. 28 We used two methods to assess the local toxicity of the NO donor.…”

“…Our results differ from previous ones in the literature. 4,16,26 Even a dose of C10 (4 mg), showing a lower enhancement effect than NOC7 (4 mg) for FD-4 (Tables 2 and3), exhibited cytotoxicity to the jejunum and colon as observed from the release of LDH and protein ( Figure 6). On the other hand, the amounts of LDH and protein released in the presence of NOC7 (4 mg) were not significantly different from those in the control (except for the protein release in the colon, which was much lower than that in the presence of C10).…”

Cell Cultures in Drug Discovery: An Industrial Perspective

“…Apart from using paracellular or transcellular markers of the functional epithelium, other techniques can be used to evaluate toxicity, e.g., MTT test, lactate dehydrogenase (LDH), morphology and confocal laser scanning [149,154,155]. The MTT test is based on the binding of the colored compound MTT to intracellular dehydrogenases; the compound is fluorescent only if the cell membrane is intact and cells are viable.…”