Polyelectrolyte Bioadhesive Delivery Systems

The mucin to which bioadhesive polymers adhere is secreted by columnar epithelial cells and is a network comprising 0.5-2% of highly-hydrated flexible glycoprotein chains [400], which contain negatively charged moieties, and are 

For bioadhesive applications, anionic polymers appear to provide the most effective balance between adhesiveness and toxicity, with carboxylic materials preferred over sulfonic polymers [400]. Polyfacrylic acid) microparticles have been identified as particularly effective bioadhesive materials [402]. Studies with poly(acrylic acid) microparticles have indicated that, while water-swollen particles exhibit good bioadhesion, dry polymer particles give no adhesion at all. In addition, adhesive strength increases as the degree of ionization of the polymer is increased [402]. Thus the expanded nature of the polymer network is important to mucoadhesion, probably via polymer interdiffusion and entanglement with mucin [403], 

The bioadhesive characteristics of tablets for oral use made from modified starch, poly(acrylic acid), polyethylene glycol) and sodium carboxymethyl cellulose were recently investigated [406]. In this work, the force and energy adhesion were determined in vitro, and maximum adhesion times were evaluated in vivo in humans [406], In the in vitro, studies, the poly(acrylic add) gave the best performance, however in vivo bioadhesion was not strongly correletated with 

A host of bioadhesive controlled release systems have been proposed in recent years. Among the most commonly studied applications of bioadhesive materials is the area of buccal controlled delivery [408], The buccal delivery of small peptides from bioadhesive polymers was studied by Bodde and coworkers [409], and a wide range of compositions based on poly(butyl acrylate) and/or poly(acrylic acid) gave satisfactory performance. Bioadhesive poly(acrylic add)-based formulations have also been used for oral applications [402,410] for the sustained delivery of chlorothiazide [410] and for a thin bioadhesive patch for treatment of gingivitis and periodontal disease [411]. Other bioadhesive applications of polyelectrolytes include materials for ophthalmic vehicles [412,413], and systems for oral [410,414,415-419], rectal [420,421] vaginal [422] and nasal [423] drug delivery. 

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