In Vitro–in Vivo Correlation of Mucoadhesion Studies on Buccal Mucosa

Background: For the development of novel buccoadhesive formulations, their physicochemical properties, strength of the interfacial joint, and residence time on the buccal mucosa are considered as a measure for their in vivo mucoadhesive properties. Focusing on these parameters, the predictive power of established in vitro systems was assessed for mucoadhesive properties in humans using discs as the model solid dosage form. Methods: Compressed into discs, hydroxyethyl cellulose, carboxymethyl cellulose, carbopol, polycarbophil, alginate, and xanthan gum were used as model polymers. Mucosal residence time, maximum detachment force (MDF), and total work of adhesion (TWA) were determined ex vivo on the porcine buccal mucosa and in vivo on healthy volunteers. The impact of detachment velocity, humidification, and experimental set-up employed for tensile studies was examined and correlated to in vivo studies. Results: Ex vivo results for mucosal residence time showed a very high correlation (r = 0.997) with dat...