title: Comparison of the mucoadhesive properties of various polymers.
abstract: In this study the mucoadhesive potential of nineteen different, most often referred mucoadhesive polymers was evaluated and characterized by adhesion time and total work of adhesion (TWA) of the polymer to porcine small intestinal mucosa. In addition, the influence of pH of the polymer and of method of drying on adhesion was evaluated. Aqueous polymer solutions were therefore adjusted to pH 3.0 and 7.0. Solutions were either dried by lyophilization (lyo.) or precipitated (pr.) in organic solvent and air-dried. Results of this study led to the following rank order of adhesion time: chitosan-4-thiobuthylamidine pH 3 lyo. >chitosan-4-thiobuthylamidine pH 6.5 pr.>polycarbophil-cysteine pH 3 lyo.>chitosan-4-thiobuthylamidine pH 6.5 lyo.>PAA450-cysteine pH 3 lyo.>pH 7 pr.>Carbopol 980 pH 7 pr.>Carbopol 974P pH 7 pr.>polycarbophil pH 7 pr.>980 pH 3 lyo. The rank order obtained for adhesion time was in agreement with the rank order obtained for total work of adhesion. The highest mucoadhesion was shown by thiolated polymers at pH 3.0, dried by lyophilization. In contrary, polyacrylates were most mucoadhesive in form of precipitated neutral sodium salts. Other tested polymers like natural polysaccharides, cellulose derivatives, polyvinylpirrolidone and polyethylenglycole, although previously reported as good mucoadhesives, showed low to almost no mucoadhesion. The pH of polymer and drying method were found to be important factors influencing the mucoadhesive potential of polymers.
authors.affiliation: Department of Pharmaceutical Technology, Institute of Pharmacy, Leopold-Franzens University Innsbruck, Innrain 52, Josef-Möller-Haus, A-6020 Innsbruck, Austria.
authors.forename: Vjera
authors.initials: V
authors.lastname: Grabovac
authors.forename: Davide
authors.initials: D
authors.lastname: Guggi
authors.forename: Andreas
authors.initials: A
authors.lastname: Bernkop-Schnürch
mesh_terms: D000268:Adhesiveness; D000818:Animals; D048271:Chitosan / Q000737:chemistry; D003890:Desiccation; D005612:Freeze Drying; D066298:In Vitro Techniques; D007413:Intestinal Mucosa / Q000378:metabolism; D009092:Mucous Membrane; D011108:Polymers / Q000737:chemistry*; D011134:Polysaccharides / Q000737:chemistry; D013438:Sulfhydryl Compounds / Q000737:chemistry; D013552:Swine; D013718:Tensile Strength; D014014:Tissue Adhesives / Q000737:chemistry*
chemical_list: D011108:Polymers; D011134:Polysaccharides; D013438:Sulfhydryl Compounds; D014014:Tissue Adhesives; D048271:Chitosan