The oral cavity is one of the most important routes for local and systemic drug delivery, as it has a large surface, high permeability, and rich blood supply. Oral mucosal drug delivery has some advantages, such as enhancing bioavailability, preventing first-pass metabolism, reducing dose frequency, and non-invasiveness. In recent years, notable oral mucoadhesive patents were introduced to the pharmaceutical field, which indicates promising potentials for therapeutic purposes. Oral mucosal drug delivery can play a key role to deliver the biological drugs, such as antimicrobial peptides. This article gives an overview of oral mucoadhesive drug delivery systems and provides basic principles for the researchers to overcome the problems associated with the formulation design.
To create your abstract, type over the instructions in the template box below. Fonts or abstract dimensions should not be changed or altered. A novel and efficient synthesis of 2-substituted quinazolin-4(3H)-ones by the reaction of (het)arylmethanamines with isatoic anhydride
Thirteen new phenoxy-biscoumarin-N-phenylacetamide derivatives (7a-m) were designed based on a molecular hybridization approach as new α-glucosidase inhibitors. These compounds were synthesized with high yields and evaluated in vitro for their inhibitory activity against yeast α-glucosidase. The obtained results revealed that a significant proportion of the synthesized compounds showed considerable αglucosidase-inhibitory activity in comparison to acarbose as a positive control. Representatively, 2-(4-(bis(4-hydroxy-2-oxo-2H-chromen-3-yl)methyl)phenoxy)-N-(4bromophenyl)acetamide (7f), with IC 50 = 41.73 ± 0.38 µM against α-glucosidase, was around 18 times more potent than acarbose (IC 50 = 750.0 ± 10.0 µM). This compound was a competitive α-glucosidase inhibitor. Molecular modeling and dynamic simulation of these compounds confirmed the obtained results through in vitro experiments. Prediction of the druglikeness/ADME/toxicity of the compound 7f and comparison with the standard drug acarbose showed that the new compound 7f was probably better than the standard drug in terms of toxicity.
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