Synthesis and characterisation of mucoadhesive thiolated polyallylamine.

The thiolation of polyallylamine (PAAm) for use in mucoadhesive drug delivery has been achieved. PAAm was reacted with different ratios of Traut's reagent, yielding products with thiol contents ranging from 134-487µmol/g. Full mucoadhesive characterisation of the thiolated PAAm samples was conducted using swelling studies, mucoadhesive testing on porcine intestinal tissue and rheology. Both swelling and cohesive properties of the thiolated PAAm products were vastly improved in comparison to an unmodified PAAm control. The swelling abilities of the thiolated samples were high and the degree of thiolation of the products affected the initial rate of swelling. High levels of mucoadhesion were demonstrated by the thiolated PAAm samples, with adhesion times of greater than 24h measured for all three samples and, thus, thiol content did not appear to influence mucoadhesion. Rheological studies of the thiolated PAAm samples showed an increase in G' and G″ values upon the addition of a mucin solution which was not observed in the unmodified control, again highlighting the mucoadhesive interactions between these thiolated polymers and mucin. The synthesis of thiolated PAAm by reaction with Traut's reagent and resulting mucoadhesive properties demonstrates its potential for use a mucoadhesive drug delivery device.

Comparison of the mucoadhesive properties of thiolated polyacrylic acid to thiolated polyallylamine.

Synthetic polymers, polyacrylic acid (PAA) and polyallylamine (PAAm), were thiolated using different methods of thiolation. Both polymers resulted in comparable thiol contents, thus allowing for the direct comparison of mucoadhesive and cohesive properties between the well-established thiolated PAA and the more novel thiolated PAAm. Thiolation of both polymers improved the swelling ability and the cohesive and mucoadhesive properties in comparison to unmodified control samples. In this study, it was shown that the swelling abilities of the thiolated PAAm sample were far greater than that of the thiolated PAA sample which, in turn, affected the drug release profile of the thiolated PAAm sample. Importantly, however, the mucoadhesive properties of thiolated PAAm were equivalent to that of the thiolated PAA sample as demonstrated by both the adhesion times on porcine intestinal tissue as measured by the rotating cylinder method and by rheological studies with a mucin solution. This study demonstrates the potential thiolated polyallylamine has as a mucoadhesive drug delivery device.

The effect of salt and fibre direction on water dynamics, distribution and mobility in pork muscle: a low field NMR study.

The effect of salt concentration and fibre orientation on water within the meat matrix was investigated by low-field nuclear magnetic resonance (LF-NMR), water-binding capacity (WBC), diffusion studies and histological analysis. Pork M. longissimus thoracis et lumborum samples were cured with 5.7, 15.3 or 26.3% w/w NaCl at a parallel or perpendicular fibre direction. NMR transverse (T2) relaxation identified three water components (T2b, T21 and T22) which all exhibited characteristics correlated to WBC. Results indicated that T2b increases with increasing NaCl concentration. Increasing intra-myofibrillar water and decreasing extra-myofibrillar water resulted in the highest WBC. Water diffused more quickly into the extra-myofibrillar space in samples cured at a parallel fibre direction. This water remained loosely bound in samples cured with the saturated solution (26.3% w/w NaCl) leading to decreased WBC. This study provides further information on water binding within the meat matrix by applying the results of LF-NMR to traditional water-binding theories.