MODELING MUCOADHESION BY USE OF SURFACE-ENERGY TERMS OBTAINED FROM THE LEWIS-ACID LEWIS BASE APPROACH .2. STUDIES ON ANIONIC, CATIONIC, ANDUNIONISABLE POLYMERS
M. Rillosi et G. Buckton, MODELING MUCOADHESION BY USE OF SURFACE-ENERGY TERMS OBTAINED FROM THE LEWIS-ACID LEWIS BASE APPROACH .2. STUDIES ON ANIONIC, CATIONIC, ANDUNIONISABLE POLYMERS, Pharmaceutical research, 12(5), 1995, pp. 669-675
Surface energies of carbopol, chitosan, hydroxypropyl cellulose (HPC)
and poly(HEMA) were assessed from contact angle and surface tension ex
periments. The surface energy was considered in terms of an apolar Lif
shitz-van der Waals term and a polar acid-base term, which in turn is
divided into electron donor and electron receptor (Lewis acid-Lewis ba
se) contributions. Using these surface energy terms the interaction of
dry and hydrated polymer with mucin in the presence of either artific
ial gastric or intestinal fluid, or saline was predicted. The predicti
ons were related to measured forces of detachment. There was a signifi
cant difference between the surface energy on dry and hydrated HPC and
also for carbopol; for the other polymers either the surface energy o
f the hydrated material was not detectable, or the effect of hydration
was minimal. There were good correlations between mucoadhesive streng
th and the calculated free energies of interaction between mucin and p
olymer in the presence of each of the fluids, for each individual poly
mer. Thus, two trends were observed, one for unionisable and the other
for ionisable polymers. It is argued that the increased mucoadhesion
seen with ionisable polymers (compared with the predicted value based
on results of unionisable polymers) is a direct result of the ionic in
teraction. No attempt has been made to correct for the ionisation effe
ct, but the surface energy predictions provide insight into the mechan
ism of the mucoadhesion process. This approach is useful for understan
ding and predicting interactions between different materials and biolo
gical components.