Mucoadhesive buccal films based on a graft co-polymer - A mucin-retentive hydrogel scaffold

Eur J Pharm Sci. 2020 Jan 15:142:105142. doi: 10.1016/j.ejps.2019.105142. Epub 2019 Nov 7.

Abstract

From a patient-centric perspective, oromucosal drug delivery is highly attractive due to the ease of administration without the need of swallowing, and improved patient safety. The aim of the presented work was to prepare a buccal film using a self-forming micellar drug solubiliser as the film matrix, combining it with a mucoadhesive polymer for an enhanced retention on the buccal mucosa. Specifically, we propose the use of a graft co-polymer (Soluplus®), as a solubiliser and film former, supplemented with polymers with more hydrophilic properties and known mucoadhesive properties; hydroxypropyl methylcellulose (HPMC) or modified hydroxypropyl pea starch (Lycoat®). The film was manufactured by the solvent casting method. The resulting dual polymer film containing HPMC exhibited resistance to erosion and mucoadhesive properties superior to the control films of single polymers. In an in vitro oral cavity model, these properties were shown to correlate with increased residence time on simulated oral mucosa. Furthermore, all films containing the graft co-polymer showed similar permeability characteristics of furosemide towards buccal TR146 epithelial cells. This work illustrated that it is possible to manufacture dry, solid, dual polymer films containing an advanced drug delivery system with a cheap and simple method. The combination of a graft co-polymer with a mucoadhesive polymer transform into drug solubilising micelles in a mucin-retentive hydrogel scaffold with longer retention time on buccal mucosa for safe and enhanced advanced formulation.

Keywords: Buccal permeability; Furosemide; HPMC; Lycoat®; Mucoadhesion; Soluplus®; Solvent casting; TR146 cells.

MeSH terms

  • Adhesiveness
  • Administration, Buccal
  • Animals
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical / methods
  • Drug Delivery Systems / methods
  • Drug Liberation / drug effects
  • HT29 Cells
  • Humans
  • Hydrogels / chemistry*
  • Hypromellose Derivatives / chemistry
  • Micelles
  • Mouth Mucosa / drug effects
  • Mucins / chemistry*
  • Permeability / drug effects
  • Polyethylene Glycols / chemistry
  • Polymers / chemistry*
  • Polyvinyls / chemistry
  • Swine

Substances

  • Hydrogels
  • Micelles
  • Mucins
  • Polymers
  • Polyvinyls
  • polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer
  • Hypromellose Derivatives
  • Polyethylene Glycols