In vitro and ex vivo evaluation of bilayered effervescent microenvironmental pH modifying buccal films with saquinavir

Buccal delivery of saquinavir has the advantage to bypass hepatic first-pass metabolism associated with oral administration. Local microenvironmental pH (pHM) modification at buccal mucosa might increase absorption by balancing solubility and partition into mucosa. The present study aimed evaluate a novel pHM modifying film using effervescence, as well elucidate relationship between permeation released from films. Hydroxypropyl methylcellulose-based films were prepared: 1) bilayered effervescent composed an alkaline layer containing malic acid, 2) monolayered acid (pHM film), 3) saquinvir (control). release these across porcine mucosae evaluated. led decrease in 6.8 3.0 after 5.5 min, while had initial (from 4.0) caused co-release subsequent 4.0 5.9) carbonate within 15 min. Saquinavir faster than film. However, higher mucosal accumulation was observed for This could be attributed concentration ionized specie tissue partitioning unionized saquinavir, respectively. These results suggest that is potential formulation strategy saquinavir.