Cyclic anhydrides are potent tools for bioconjugation; therefore, they are broadly used in the functionalization of biomolecules and carriers. The pH-dependent stability and reactivity, as well as the physical properties, can be tuned by the structure of the cyclic anhydride used; thus, their application in smart delivery systems has become very important. This review intends to cover the last updates in the use of cyclic anhydrides as pH-sensitive linkers, their differences in reactivity, and the latest applications found in bioconjugation chemistry or chemical biology, and when possible, in drug delivery.