Role of physicochemical properties of some grades of hydroxypropyl methylcellulose on in vitro mucoadhesion

Abstract

Relationships between physicochemical properties of hydroxypropyl methylcellulose (HPMC) compacts and their in vitro mucoadhesive performances were investigated in this study. Some commercial grades of HPMC (K3, E3, E5, E50, K4M, E4M and K15M) were prepared into compacts, and their surface hydrophilicity and hydration behavior were characterized. The in vitro mucoadhesive performance was determined by the tensile strength between the compacts and different regions of mucosal membrane (buccal, sublingual, stomach, and intestine). Positive correlations were found between: (1) viscosity of HPMC compacts and contact angle in different simulated body fluids; (2) viscosity of HPMC compacts and in vitro mucoadhesive force; (3) contact angle and in vitro mucoadhesive force. The hydration increased with an increase in viscosity of HPMC compacts. The polar lipid content in mucosa was found to be an important factor affecting the mucoadhesion. Lower polar lipid amount in the mucosal membrane promoted the rate of mucoadhesive force with the increasing viscosity of HPMC. The mucoadhesive mechanism of various grades of HPMC compacts were studied using the thermodynamic analysis of Lifschitz-van der Waals (LW) interaction and Lewis acid-base (AB) interactions. The total free energy of adhesion (ΔGTOT) provided a prediction of an overall tendency of mucoadhesion, and deviated from the measured mucoadhesive force.