The aim of this work was to develop a novel and more efficient platform for sublingual drug delivery\nusing mosapride citrate (MSP) as a model drug. The engineering of this delivery system had two\nstages, the first stage was tuning of MSP physicochemical properties by complexation with pure\nphosphatidylcholine or phosphatidylinositol enriched soybean lecithin to form MSP-phospholipid complex\n(MSP-PLCP). Changes in physicochemical properties were assessed and the optimum MSP-PLCP\nformula was then used for formulation into a flushing resistant platform using two mucoadhesive polymers;\nsodium alginates and sodium carboxymethylcellulose at different concentrations. Design of\nexperiment approach was used to characterize and optimize the formulated flushing resistant platform.\nThe optimized formulation was then used in a comparative pharmacokinetics study with the market\nformulation in human volunteers. Results showed a marked change in MSP physicochemical properties\nof MSP-PLCP compared to MSP. Addition of mucoadhesive polymers to flushing resistant platform at\nan optimum concentration balanced between desired mucoadhesive properties and a reasonable drug\nrelease rate. The optimized formulation showed significantly a superior bioavailability in humans when\ncompared to the market sublingual product. Finally, the novel developed sublingual flushing resistant\nplatform offers a very promising and efficient tool to extend the use of sublingual route and widen its\napplications.
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