title: Synthesis and characterisation of mucoadhesive thiolated polyallylamine.
abstract: 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.
authors.affiliation: Pharmaceutical and Molecular Biotechnology Research Centre, Department of Chemical and Life Sciences, Waterford Institute of Technology, Waterford, Ireland. Electronic address: sduggan@wit.ie.
authors.forename: Sarah
authors.initials: S
authors.lastname: Duggan
authors.affiliation: Pharmaceutical and Molecular Biotechnology Research Centre, Department of Chemical and Life Sciences, Waterford Institute of Technology, Waterford, Ireland.
authors.forename: Helen
authors.initials: H
authors.lastname: Hughes
authors.affiliation: Pharmaceutical and Molecular Biotechnology Research Centre, Department of Chemical and Life Sciences, Waterford Institute of Technology, Waterford, Ireland.
authors.forename: Eleanor
authors.initials: E
authors.lastname: Owens
authors.affiliation: Pharmaceutical and Molecular Biotechnology Research Centre, Department of Chemical and Life Sciences, Waterford Institute of Technology, Waterford, Ireland.
authors.forename: Elaine
authors.initials: E
authors.lastname: Duggan
authors.affiliation: Pharmaceutical and Molecular Biotechnology Research Centre, Department of Chemical and Life Sciences, Waterford Institute of Technology, Waterford, Ireland.
authors.forename: Wayne
authors.initials: W
authors.lastname: Cummins
authors.affiliation: Pharmaceutical and Molecular Biotechnology Research Centre, Department of Chemical and Life Sciences, Waterford Institute of Technology, Waterford, Ireland.
authors.forename: Orla
authors.initials: O
authors.lastname: O' Donovan
mesh_terms: D000268:Adhesiveness; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D007413:Intestinal Mucosa / Q000378:metabolism; D009077:Mucins / Q000378:metabolism; D011073:Polyamines / Q000138:chemical synthesis / Q000737:chemistry*; D011108:Polymers / Q000138:chemical synthesis / Q000737:chemistry; D012212:Rheology; D013438:Sulfhydryl Compounds / Q000138:chemical synthesis / Q000737:chemistry*; D013552:Swine; D013997:Time Factors
chemical_list: D009077:Mucins; D011073:Polyamines; D011108:Polymers; D013438:Sulfhydryl Compounds; C063994:polyallylamine
keywords: Mucoadhesion; Polyallylamine; Thiolation; Traut’s reagent