On the role of excipients and their future development

Beijing Royal School, Beijing, 102209, China

Abstract

Excipients are inactive substances that are included in pharmaceutical formulations alongside active ingredients. These substances are added to pharmaceutical products for various purposes, including improving stability, enhancing bioavailability, aiding in the manufacturing process, enhancing the appearance or taste, and facilitating administration or delivery of the active ingredient. We summarized a recent study published in science. This work suggests a systematic method to identify such active “inactive ingredients,” including the detection of allergenic and immunogenic properties. The examined excipient activity by combining large-scale computational screening with targeted experimental testing. They identified 38 excipients with activities against 44 targets. Although most excipients deserve their status as inert, many approved excipients may directly modulate physiologically relevant targets. This review increases our understanding of the relationship between drug excipients and active sites and provides more comprehensive theoretical support for future excipient selection.