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Oral drug delivery technology is mainly provided in the form of solid oral dosage forms (SODF) that have to be swallowed intact and move throughout the oro-esophageal system to release the drug content in the stomach or intestine. As there is growing evidence for an increasing prevalence of impaired swallowing functions in certain diseases, multimorbidity and advanced age, predictive in vitro methods for the oro-esophageal gliding behavior of SODF would be very useful. The gliding performance of different SODF polymer films was investigated across an artificial mucous layer using a versatile in vitro gliding system. In a first phase, the system measures the force required to move the polymer surface when placed in contact with the mucin layer and, in a second phase, the resistance behavior over a defined length. The obtained results showed that comprehensive gliding profiles could be obtained depending on the polymer film tested. The carnauba wax and PEG coatings required lower gliding peak forces and showed poor gliding resistance, which is indicative of free gliding capacity. In contrast, HPMC, PVP and gelatin coatings required higher gliding forces and exhibited greater resistance due to an adhesive interaction with the artificial mucous layer. The obtained profiles correlate with prior in vitro data during polymer gliding evaluations on mucosal membranes., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Predicting the potential for unintended adhesion of solid oral dosage forms (SODF) to mucosal tissue is an important aspect that should be considered during drug product development. Previous investigations into low strength mucoadhesion based on particle interactions methods provided evidence that rheological measurements could be used to obtain valid predictions for the development of SODF coatings that can be safely swallowed. The aim of this second work was to estimate the low mucoadhesive strength properties of different polymers using in vitro methods based on mechanical forces and to identify which methods are more precise when measuring reduced mucoadhesion. Another aim was to compare the obtained results to the ones achieved with in vitro particle interaction methods in order to evaluate which methodology can provide stronger predictions. The combined results correlate between particle interaction methods and mechanical force measurements. The polyethylene glycol grades (PEG) and carnauba wax showed the lowest adhesive potential and are predicted to support safe swallowing. Hydroxypropyl methylcellulose (HPMC) along with high molecular grades of polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA) exhibited strong in vitro mucoadhesive strength. The combination of rheological and force tensiometer measurements should be considered when assessing the reduced mucoadhesion of polymer coatings to support safe swallowing of SODF., (Copyright © 2018 Elsevier B.V. All rights reserved.)

The oral cavity is frequently used to administer pharmaceutical drug products. This route of administration is seen as the most accessible for the majority of patients and supports an independent therapy management. For current oral dosage forms under development, the prediction of their unintended mucoadhesive properties and esophageal transit profiles would contribute for future administration safety, as concerns regarding unintended adhesion of solid oral dosage forms (SODF) during oro-esophageal transit still remain. Different in vitro methods that access mucoadhesion of polymers and pharmaceutical preparations have been proposed over the years. The same methods might be used to test non-adhesive systems and contribute for developing safe-to-swallow technologies. Previous works have already investigated the suitability of non-animal derived in vitro methods to assess such properties. The aim of this work was to review the in vitro methodology available in the scientific literature that used animal esophageal tissue to evaluate mucoadhesion and esophageal transit of pharmaceutical preparations. Furthermore, in vivo methodology is also discussed. Since none of the in vitro methods developed are able to mimic the complex swallowing process and oro-esophageal transit, in vivo studies in humans remain as the gold standard., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Solid oral dosage forms (SODF) are drug vehicles commonly prescribed by physicists in primary and secondary cares, as they are the most convenient for the patient and facilitate therapy management. Concerns regarding unintended adhesion of SODF during oro-esophageal transit remain, especially in multimorbid patients, bedridden patients and patients suffering from dysphagia. Hence, this factor should be considered during the development of SODF, and more attention should be given on the design of appropriate surface conditions considering patients with swallowing problems. The aim of this work was to estimate the low mucoadhesion strength of different pharmaceutical polymers frequently used in coating technologies, since this property is thought to have impact on the mucoadhesive profile of SODF during oro-esophageal transit. In an approach using in vitro methods based on particle interactions, polyethylene glycol grades (PEG) showed the lowest interaction forces suggesting a more favorable in vivo performance than hydroxypropyl methylcellulose (HPMC), which was found to have the highest particle interaction. Preference should be given to coating formulations with lower concentrations of polymer and grades with low molecular weight. In addition, rheological measurements should be adopted when targeting poor mucoadhesive polymers., (Copyright © 2018 Elsevier B.V. All rights reserved.)