title: An evaluation of the adhesion of solid oral dosage form coatings to the oesophagus.
abstract: There is a requirement for the development of oral dosage forms that are adhesive and allow extended oesophageal residence time for localised therapies, or are non-adhesive for ease of swallowing. This study provides an initial assessment of the in vitro oesophageal retention characteristics of several widely utilised pharmaceutical coating materials. To this end, a previously described apparatus has been used to measure the force required to pull a coated disc-shaped model tablet across a section of excised oesophageal tissue. Of the materials tested, the well-studied mucoadhesive polymer sodium alginate was found to be associated with significant oesophageal adhesion properties that was capable of 'self-repairing'. Hydroxypropylmethylcellulose exhibited less pronounced bioadhesive behaviour and blending this with plasticiser or with low molecular weight polymers and surfactants did not significantly affect this. Low molecular weight water soluble polymers, were found to behave similarly to the uncoated glass control disc. Polysorbates exhibited bioadhesion behaviour that was majorly influenced by the nature of the surfactant. The insoluble polymer ethylcellulose, and the relatively lipophilic surfactant sorbitan monooleate were seen to move more readily than the uncoated disc, suggesting that these may have a role as 'easy-to-swallow' coatings.
authors.affiliation: Drug Delivery Research Group, School of Pharmacy and Biomolecular Sciences, University of Brighton, Brighton, BN2 4GJ England, United Kingdom. Electronic address: john.smart@brighton.ac.uk.
authors.forename: John D
authors.initials: JD
authors.lastname: Smart
authors.affiliation: School of Pharmacy and Biomedical University Sciences, University of Portsmouth, Portsmouth, England, United Kingdom.
authors.forename: Sian
authors.initials: S
authors.lastname: Dunkley
authors.affiliation: School of Pharmacy and Biomedical University Sciences, University of Portsmouth, Portsmouth, England, United Kingdom.
authors.forename: John
authors.initials: J
authors.lastname: Tsibouklis
authors.affiliation: School of Medical Sciences, RMIT University, PO Box 71, Bundoora, Victoria 3083, Australia.
authors.forename: Simon
authors.initials: S
authors.lastname: Young
mesh_terms: D000269:Adhesives / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D000284:Administration, Oral; D004304:Dosage Forms; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004947:Esophagus / Q000187:drug effects / Q000378:metabolism; D005079:Excipients / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D065347:Hypromellose Derivatives / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D009061:Mouth Mucosa / Q000187:drug effects / Q000378:metabolism; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D013608:Tablets, Enteric-Coated
chemical_list: D000269:Adhesives; D004304:Dosage Forms; D005079:Excipients; D013608:Tablets, Enteric-Coated; D065347:Hypromellose Derivatives; D011092:Polyethylene Glycols
keywords: Easy-to-swallow; Mucoadhesion; Non-adhesive coatings; Oesophageal adhesion