Enhancement of Solubility and Dissolution Rate Using Tailored Rapidly Dissolving Oral Films Containing Felodipine Solid Dispersion: In Vitro Characterization and Ex Vivo Studies.

Purpose: The goal of the present investigation was to establish felodipine (FDP) solid dispersion-loaded transmucosal buccal films which may help to increase its solubility and avoid hepatic first-pass metabolism to boost its oral bioavailability leading to better treatment of hypertension. Methods: The solid dispersion was prepared using fusion method. The effect of varying ratios of poloxamer 407 on dissolution of FDP was studied. Prepared FDP solid dispersions were characterized concerning FTIR, DSC, PXRD, and SEM. Further, the standardized FDP solid dispersion was incorporated into RDOFs that were fabricated by mold casting technique. Results: SEM micrographs of RDOFs revealed the presence of FDP solid dispersion in the matrix of the polymer. Ex vivo permeation of the drug from FDP-loaded RDOF and FDP solid dispersion-loaded RDOF across porcine buccal mucosa was found to be 17.3 ± 0.11% and 84.81 ± 7.19%, respectively in 90 min. Conclusion: Obtained results conclude that the prepared FDP solid dispersion-loaded RDOFs may be a useful approach to augment the oral bioavailability of FDP by ameliorating its solubility and the rate of dissolution, and it can also reduce hepatic first-pass metabolism. [ABSTRACT FROM AUTHOR]