In Vitro-in Vivo Correlation of Mucoadhesion Studies on Buccal Mucosa.

Abstract

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. 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. Ex vivo results for mucosal residence time showed a very high correlation ( r = 0.997) with data obtained in vivo. For tensile studies, a set-up optimized for moistening the interface, speed, and alignment of the tensile force provided ex vivo results with very high correlation to in vivo experiments with r = 0.983 obtained for MDF and r = 0.973 for TWA, respectively. Experimental set-ups for the determination of mucosal residence time and tensile studies could be identified as valid methods for the development of intraoral solid dosage forms.