Oral transmucosal delivery of eletriptan for neurological diseases

Three-Dimensional Oral Mucosal Equivalents as Models for Transmucosal Drug Permeation Studies

“…Indeed, we believed that EB was a good model drug since it has a hydrophobic skeleton, but it is charged at physiological pH, being both hydrophobic and hydrophilic at the same time. We recently studied EB permeability in oral transmucosal delivery and the effects of the drug concentration, pH and with a penetration enhancer using model and ex vivo membranes (porcine and 3D commercial OME) [ 19 , 29 ]. The full-thickness model developed here showed the same cumulative drug-permeated profile as the commercial EpiOral™, suggesting that they present the same permeation barrier properties ( Figure 5 ).…”

“…It is difficult to conclude that the barrier property observed in the full-thickness model is due to the addition of the lamina propria plus epithelial barrier, since we have shown previously that the lamina propria has little influence on the EB permeation [ 19 ]. Instead, the less tight barrier observed in the split-thickness model is likely due to the reduced stratification in the epithelial layer compared to the full-thickness model ( Figure 2 and Figure 3 ).…”

“…Instead, the less tight barrier observed in the split-thickness model is likely due to the reduced stratification in the epithelial layer compared to the full-thickness model ( Figure 2 and Figure 3 ). We have previously linked increased EB permeation at pH 6.8 (i.e., charged form of EB~99%) to the presence of more hydrophilic pathways in the membrane [ 19 ], suggesting that our split-thickness model could potentially present more hydrophilic pathways. Although the split-thickness protocol represents a promising, cheaper tissue-engineering protocol, further investigations are needed to reach the same barrier properties as the commercial EpiOral™, considered as the reference model for a drug permeation membrane.…”

“…The samples collected from the permeation experiments were analyzed with HPLC-UV (Agilent 1100 Series, Agilent Technologies, Mulgrave, Australia) using a method previously reported [ 19 ]. Briefly, a SVEA HPLC C 18 column (4.6 × 100 mm, 3.5 m, Nanologica, Södertälje, Sweden) with a Phenomenex SecurityGuard precolumn with cartridges C 18 4 × 3.0 mm ID (AJO-4287 Phenomenex, Værløse, Denmark) was used.…”

Buccal Permeation of Polysaccharide High Molecular Weight Compounds: Effect of Chemical Permeation Enhancers

“…The model membrane used for this kind of experiment should be, however, very well characterized. In the literature, there is some evidence indicating that the porcine esophageal mucosa is a relevant model of the buccal epithelium [ 27 , 28 , 29 , 30 , 31 , 32 , 33 , 34 , 35 , 36 ]. However, most of these studies have been performed with low MW compounds, and these results cannot be directly extrapolated to hydrophilic macromolecules, probably characterized by different penetration pathways [ 37 ].…”