Dwivedi et al._Pharmaceutics_raw data (6-17-25).xlsx

The oral cavity represents a convenient route of administration for drugs that exhibit significant hepatic first-pass extraction. In this study, mucosal permeation properties of selected active pharmaceutical ingredients (APIs) incorporated in oral cavity drug products that are approved by the U.S. Food and Drug Administration were quantified using the human-derived sublingual HO-1-u-1 and buccal EpiOral™ in vitro tissue models. Epithelial barrier properties were monitored using propranolol and Lucifer Yellow as prototypic transcellular and paracellular markers. APIs were dissolved in artificial saliva, pH 6.7, and transepithelial flux from the apical to the basolateral compartment was quantified using HPLC. Experimental permeation data collected for selected APIs in FDA-approved oral cavity products will serve as a training set to aid development of predictive computational models for improving algorithms that describe drug absorption from the oral cavity. Following a robust in vitro – in vivo correlation analysis, it is expected that such innovative in silico modeling strategies will accelerate development of generic oral cavity products by facilitating the utility of model-integrated evidence to support decision making in generic drug development and regulatory approval