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Development of nanostructured mucoadhesive systems containing the epoxide hydrolase inhibitor (TPPU) for buccal use

Grant number: 16/11792-3
Support type:Scholarships in Brazil - Post-Doctorate
Effective date (Start): November 01, 2016
Effective date (End): July 31, 2017
Field of knowledge:Biological Sciences - Pharmacology
Principal Investigator:Marcelo Henrique Napimoga
Grantee:Nathalie Ferreira Silva de Melo
Home Institution: Centro de Pesquisas Odontológicas São Leopoldo Mandic. Faculdade São Leopoldo Mandic (SLMANDIC). Sociedade Regional de Ensino e Saúde S/S Ltda (SRES). Campinas , SP, Brazil

Abstract

Recently the mucoadhesive systems for drug delivery have been highlighted due to the direction and more specific retention of the drug incorporated into the system. These formulations when combined with nanotechnology enable the control of drug release, and are used as a strategy to increase the bioavailability. The buccal route for drug delivery has shown to be very attractive as the major vasculature facilitates the absorption process and avoids first pass metabolism. However, buccal route has clearance mechanisms such as saliva and mucus production, and to prolong the residence time of formulations in this route nanostructured mucoadhesive systems are proposed. The epoxyeicosatrienoic acid (EET) is derived from arachidonic acid metabolism and has been demonstrated its activity in the control of inflammation, angiogenesis and cardiovascular function, but its presence in the tissues is eliminated by epoxide enzyme activity hydrolase soluble (sEH). In recent years there have been investigated sEH stable inhibitors, such as 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) (TPPU) as a strategy to increase the levels of EET in tissues, representing an alternative therapy for various diseases. Thus, sEH inhibitors could have a beneficial effect may reduce the inflammatory process. Thus, the objective of present work is to develop (preparation and characterization) a nanostructured mucoadhesive formulation for buccal release of sEH inhibitor (TPPU) aiming a new system for clinical use in treating inflammatory diseases. Because it is a new formulation is also intended to evaluate them for in vitro cytotoxicity.