Design, characterization, and biological assessment of a buccal SNEDDS gel for improved rivaroxaban delivery

In the present study, a mucoadhesive buccal gel incorporating a rivaroxaban-loaded self-nanoemulsifying drug delivery system (RVN-SNEDDS) was formed and optimized to enhance drug dissolution, mucosal permeation, and systemic bioavailability.

RVN-SNEDDS was developed and enclosed into buccal gels formulated with carbomer, hyaluronic acid, or their combination. A factorial design method was applied to investigate the influence of polymer system and concentration on mucoadhesive strength, rheological properties, spreadability, and <i>in vitro</i> drug release. The optimized formulation showed rapid initial drug release, with about one-third of the drug released within the first 5 min and more than 85 ± 4.23% released within 30 min, followed by sustained release behavior. <i>Ex vivo</i> permeation studies showed significantly increase in rivaroxaban transport across buccal mucosa in comparison to conventional formulations. <i>In vivo</i> pharmacokinetic evaluation in rabbits revealed a faster onset of action and a marked increase in systemic bioavailability in compare to the marketed oral tablet.