In vitro apparent permeability assessment and in vivo pharmacokinetics of sesquiterpene lactones isolated from Mikania nummularia DC.

• Grant number: 25/08091-2
• Support Opportunities: Scholarships abroad - Research Internship - Doctorate
• Start date: January 12, 2026
• End date: December 19, 2026
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: João Henrique Ghilardi Lago
• Grantee: Marina de Monroe Gonçalves
• Supervisor: Ana Cristina Bairrada Fortuna
• Host Institution: Centro de Ciências Naturais e Humanas (CCNH). Universidade Federal do ABC (UFABC). Ministério da Educação (Brasil). Santo André , SP, Brazil
• Institution abroad: Universidade de Coimbra (UC), Portugal
• Associated to the scholarship: 23/14422-6 - Specialized metabolites from Mikania nummularia DC. - structural characterization, evaluation of antiparasitic potential in vitro and in vivo, and determination of pharmacokinetic parameters, BP.DR

Abstract

Neglected tropical diseases (NTDs), such as Chagas disease and schistosomiasis, remain a global challenge due to the scarcity of effective treatments and the emergence of resistance to available drugs. In this context, sesquiterpene lactones (SLs) have emerged as a promising class of bioactive compounds with significant antiparasitic potential. This project aims to investigate the in vitro and in vivo pharmacokinetic parameters of SLs isolated from Mikania nummularia, a phytochemically unexplored species, in order to expand current knowledge regarding their bioavailability and behavior in biological systems. Initially, Parallel Artificial Membrane Permeability Assay (PAMPA) models will be employed to assess intestinal absorption (PAMPA-TGI) and blood-brain barrier permeability (PAMPA-BBB) of the compounds under investigation. Subsequently, selected compounds will be subjected to in vivo pharmacokinetic studies following oral and intravenous administration. Key pharmacokinetic parameters such as area under the curve (AUC), maximum plasma concentration (Cmax), time to reach maximum concentration (Tmax), half-life (T1/2), and mean residence time (MRT) will be determined. The data obtained will contribute to the advancement of these substances as potential antiparasitic drug candidates, providing essential information for future in vivo antiparasitic efficacy studies. (AU)