Study of apparent permeability in Caco-2 cells of drug candidates with potential nootropic activity

• Grant number: 19/09444-5
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Effective date (Start): February 01, 2020
• Effective date (End): December 31, 2020
• Field of knowledge: Biological Sciences - Pharmacology
• Principal Investigator: Rosangela Gonçalves Peccinini
• Grantee: Vítor Yukio Kobashikawa
• Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

The improvement of technologies in analysis and synthesis, structural characterization and the introduction of combinatorial chemistry promoted an acceleration in obtaining new synthetic compounds. Early evaluations of pharmacokinetic properties through in vitro assays provide notions of absorption, allowing preliminary screening by excluding less promising candidates and direct investments to the best profile compounds. Currently, permeability studies have several in vitro models to examine the permeability of new compounds; a commonly used is the Caco-2 cells monolayer model. Worldwide, the life expectancy of the population has increased significantly in recent years and the use of nootropic drugs can bring these individuals a greater quality of life. Therefore, the availability of new compounds for pharmacotherapy with this therapeutic purpose is urgent. Researchers from UNIFESP have achieved promising results regarding their nootropic activity of new compounds, already published in a known worldwide journal. However, the pharmacokinetic properties evaluation has not been performed yet. This proposal assembles projects of new molecules synthesis to work in the evaluation of these new compounds which have a potential application on central nervous system disorders and approaches in vitro apparent permeability assays in Caco-2. In addition, this proposal aims to assist the development of pharmaceutical products, whose therapeutic application results in a favorable clinical outcome, supporting the increase of life expectancy and quality of life.