Establishment of PK-PD model in anti-inflammatory active components in Inula cappa extract based on lipopolysaccharide-induced in vitro inflammation model

Inula cappa extract contains several anti-inflammatory active components, but the relationship between their cellular pharmacokinetics and anti-inflammatory efficacy had not been characterized. This study used an LPS-induced in vitro inflammation model in RAW264.7 cells to compare the pharmacokinetics of five active components (including luteolin and various caffeoylquinic acids) between normal and inflamed cells, then built a combined pharmacokinetic-pharmacodynamic model using inflammatory markers NO and TNF-alpha via the Phoenix WinNonlin platform. Inflammatory cells showed altered uptake and absorption kinetics of the active components compared with normal cells, and the resulting PK-PD models linked the anti-inflammatory effect to down-regulation of NO and TNF-alpha secretion. The study suggests these two inflammatory markers may serve as therapeutic targets for Inula cappa’s anti-inflammatory active components.