Cm. Lehr et al., A SURFACE-ENERGY ANALYSIS OF MUCOADHESION .2. PREDICTION OF MUCOADHESIVE PERFORMANCE BY SPREADING COEFFICIENTS, European journal of pharmaceutical sciences, 1(1), 1993, pp. 19-30
Mucoadhesion refers to the adhesion of polymeric materials to mucosal
tissues. Some mucoadhesive polymers show appreciable binding to mucus
even when hydrated and in the presence of an interstitial aqueous medi
um. The mucoadhesive performance (i.e. binding strength) is expected t
o depend on the interfacial energy thermodynamics in a three phase (so
lid-liquid-solid) system. According to known theories, such a system c
an be described in terms of spreading coefficients which are given by
the free surface energy of each phase. Dispersion (alpha) and polar (b
eta) surface energy parameters were available from previously reported
contact angle measurements of captive air/octane bubbles on polymeric
hydrogels and pig intestinal mucosa immersed in aqueous test media. I
t was found that individual spreading coefficients, as calculated from
these surface energy parameters by the geometric mean equation, can b
e combined to one single parameter, called combined spreading coeffici
ent S(c). The latter is defined by the geometric mean of the polymer s
preading coefficient and the Griffith fracture energy. This criterion
provided a good correlation between predicted and measured mucoadhesiv
e performance under various experimental circumstances. In its present
form, this approach is based only on dispersion and polar surface ene
rgy components, without taking into account other forces due to ionic
interactions, hydrogen bonding or acid-base interactions and eventual
polymer chain interpenetration. Nevertheless, correct predictions were
obtained. It is therefore concluded that the formation of a mucoadhes
ive bond is primarily governed by the aforementioned surface energy ef
fects and spreading processes. The surface energy concept provides use
ful information for the search for better mucoadhesive materials and t
he identification of favored target sites in the human body for mucoad
hesive drug delivery systems.