How does food and an animal’s sex affect gastrointestinal efflux transporters?

Written by Francesca Gavins

The extent of drug bioavailability can vary between and within subjects, which can affect the safety and efficacy of oral drug products in patients. Patient-specific factors such as sex, diet and the timing of drug administration after a meal can alter key drug pharmacokinetic properties.

Here, the Biopharmaceutics researchers from the Basit Research group in UCL School of Pharmacy and Shenzhen investigate the influence of the type of food, an animal model’s sex (male and female) and postprandial time on three key efflux transporters and hormones. P-gp, breast cancer resistant protein (BCRP) and multidrug resistant protein 2 (MRP2) are clinically relevant efflux pumps with a wide range of substrates.

Our study found that in male rats, a fibre meal caused an increase in the gastrointestinal hormone cholecystokinin (CCK) and a decrease in the sex hormone testosterone. In contrast, a housing meal caused a decrease in the CCK and an increase in testosterone. However, no significant changes were seen in female rats. Interestingly, the fibre meal increased the expression of P-gp, BCRP and MRP2 in both sexes. A deeper understanding of the modulation of efflux transporters by sex, food intake and postprandial time can improve our understanding of inter- and intra-variability in the absorption of drug substrates.

Read our article here https://doi.org/10.3390/pharmaceutics13111789