Mucoadhesive hydrogels for buccal drug delivery: In vitro-in vivo correlation study

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 142; pp. 498 - 505
• Main Authors: Baus, Randi Angela, Zahir-Jouzdani, Forouhe, Dünnhaupt, Sarah, Atyabi, Fatemeh, Bernkop-Schnürch, Andreas
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.09.2019
• Subjects: Buccoadhesion; Hydrogel properties; IVIVC; Mucosal residence time; Tensile studies; Texture analysis; Hydrogel properties; Texture analysis; Buccoadhesion; Mucosal residence time; IVIVC; Tensile studies
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2019.07.019

[Display omitted] It was the aim of this study to assess in vitro methods for the characterization of mucoadhesive hydrogels for their potential to predict the residence time on human buccal mucosa. Mixtures of hydrogels comprising hydroxyethyl cellulose (HEC), sodium carboxymethyl cellulose (CMC), xanthan gum (XTGM), hyaluronic acid sodium salt (HA), sodium alginate (ALG), carbopol (CP) as well as polycarbophil (PCP) and porcine mucus were analysed for relative rheological synergism. Furthermore, hydrogels were characterized for their texture and mechanical properties. For the assessment of mucoadhesive strength of formulations tensile studies were performed on porcine buccal mucosa. To facilitate a direct comparability of data the residence time of stained hydrogels was determined ex vivo on porcine buccal mucosa and in the oral cavity of volunteers. The extent of relative rheological synergism was in good agreement with data from in vivo residence time studies. Results of tensile studies were further effected by textural properties of hydrogels leading to a restricted correlation with data from the in vivo experiment. The resistance towards removal by artificial saliva flow ex vivo revealed the highest correlation to the in vivo experiment with increasing mucosal residence time in the rank order CP < HEC, HA, ALG, PCP < CMC < XTGM. This overview of measurement principles to predict the residence time of hydrogels for buccal application in humans may be a potent tool for the development of semisolid intraoral formulations.