Unexpected Bioactivities of Drug Excipients

Excipients are major components of formulated drugs. These are materials included to promote stability or to control the bioavailability of active drug substances. They are assumed to be biologically inert.

Biologically active excipients may be concerning if they are associated with adverse human health effects and if systemic exposures reach active concentrations. Given the number of prescriptions taken, especially by older adults, and the fact that many excipients are included in foods and over the counter supplements, this may be a bigger problem than previously recognized.

Non-animal methods have been used to characterize several common drug excipients. These methods use computational methods, in vitro testing and phenotypic profiling to suggest and confirm effects on human targets and cell-based systems.

In order to make profiling results more accessible to exploration by researchers, we are developing interactive visualizations. These tools can facilitate comparative studies of different excipients and support the development of safer drug formulations.

See our case study, Challenging Assumptions About “Inactive Ingredients”, on selected excipients tested in human primary cell-based models based on the paper by Pottel et al., in Science.